Synthesis and optical limiting properties of new lanthanide bis-and tris-phthalocyanines
- Sekhosana, Kutloana Edward, Manyeruke, Meloddy Hlatini, Nyokong, Tebello
- Authors: Sekhosana, Kutloana Edward , Manyeruke, Meloddy Hlatini , Nyokong, Tebello
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/240063 , vital:50795 , xlink:href="https://doi.org/10.1016/j.molstruc.2016.05.068"
- Description: This manuscript reports on syntheses of new multi-decker phthalocyanines, namely: bis-{2,3,9,10,16,10,16,17,23,24-octa(4-tertbutylphenoxy) phthalocyaninato} cerium(III) (2), tris-{2,3,9,10,16,10,16,17,23,24-octa(4-tertbutylphenoxy) phthalocyaninato} dicerium(III) (4) and bis-{2,3,9,10,16,10,16,17,23,24-octa(4-tertbutylphenoxy) phthalocyaninato} gadolinium(III) (5). Complex 4 which is a tris phthalocyanine showed better nonlinear optical behavior in solution than 2 which is a bis phthalocyanine, both containing the same central metal, Ce. All the three molecules possess good optical limiting properties judged by the limiting threshold values which ranged from 0.04 to 0.09 J cm−2 with complex 5 embedded in thin films, showing the lowest value of 0.04 J cm−2. Furthermore, nonlinear optical processes responsible for reverse saturable absorption data are investigated.
- Full Text:
- Date Issued: 2016
- Authors: Sekhosana, Kutloana Edward , Manyeruke, Meloddy Hlatini , Nyokong, Tebello
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/240063 , vital:50795 , xlink:href="https://doi.org/10.1016/j.molstruc.2016.05.068"
- Description: This manuscript reports on syntheses of new multi-decker phthalocyanines, namely: bis-{2,3,9,10,16,10,16,17,23,24-octa(4-tertbutylphenoxy) phthalocyaninato} cerium(III) (2), tris-{2,3,9,10,16,10,16,17,23,24-octa(4-tertbutylphenoxy) phthalocyaninato} dicerium(III) (4) and bis-{2,3,9,10,16,10,16,17,23,24-octa(4-tertbutylphenoxy) phthalocyaninato} gadolinium(III) (5). Complex 4 which is a tris phthalocyanine showed better nonlinear optical behavior in solution than 2 which is a bis phthalocyanine, both containing the same central metal, Ce. All the three molecules possess good optical limiting properties judged by the limiting threshold values which ranged from 0.04 to 0.09 J cm−2 with complex 5 embedded in thin films, showing the lowest value of 0.04 J cm−2. Furthermore, nonlinear optical processes responsible for reverse saturable absorption data are investigated.
- Full Text:
- Date Issued: 2016
Synthesis and biological evaluation of bis-N2, N2′-(4-hydroxycoumarin-3-yl) ethylidene]-2, 3-dihydroxysuccinodihydrazides
- Manyeruke, Meloddy H, Tshiwawa, Thendamudzimu, Hoppe, Heinrich, Isaacs, Michelle, Seldon, Ronnett, Warner, Digby F, Krause, Rui W M, Kaye, Perry T
- Authors: Manyeruke, Meloddy H , Tshiwawa, Thendamudzimu , Hoppe, Heinrich , Isaacs, Michelle , Seldon, Ronnett , Warner, Digby F , Krause, Rui W M , Kaye, Perry T
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193430 , vital:45331 , xlink:href="https://doi.org/10.1016/j.bmcl.2019.126911"
- Description: A series of N2,N2′-bis[4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccino-hydrazides, containing 4-hydroxycoumarin, hydrazine and tartaric acid moieties, have been prepared and examined for possible biological activity. Several of these compounds exhibit promising HIV-1 integrase inhibition (IC50 = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity.
- Full Text:
- Date Issued: 2020
- Authors: Manyeruke, Meloddy H , Tshiwawa, Thendamudzimu , Hoppe, Heinrich , Isaacs, Michelle , Seldon, Ronnett , Warner, Digby F , Krause, Rui W M , Kaye, Perry T
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193430 , vital:45331 , xlink:href="https://doi.org/10.1016/j.bmcl.2019.126911"
- Description: A series of N2,N2′-bis[4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccino-hydrazides, containing 4-hydroxycoumarin, hydrazine and tartaric acid moieties, have been prepared and examined for possible biological activity. Several of these compounds exhibit promising HIV-1 integrase inhibition (IC50 = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity.
- Full Text:
- Date Issued: 2020
The crystal structure of 2-oxo-2H-chromen-4-yl acetate, C11H8O4
- Hulushe, Siya T, Manyeruke, Meloddy H, Hosten, Eric C, Kaye, Perry, Watkins, Gareth M
- Authors: Hulushe, Siya T , Manyeruke, Meloddy H , Hosten, Eric C , Kaye, Perry , Watkins, Gareth M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194048 , vital:45418 , xlink:href="https://doi.org/10.1515/ncrs-2019-0698"
- Description: C11H8O4, monoclinic, P21/c (no. 14), a = 4.5947(2) Å, b = 10.5414(3) Å, c = 19.1611(7) Å, β = 94.084(2)°, V = 925.70(6) Å3, Z = 4, Rgt(F) = 0.0376, wRref(F 2) = 0.1109,T = 200(2) K.CCDC no.: 1906383
- Full Text:
- Date Issued: 2020
- Authors: Hulushe, Siya T , Manyeruke, Meloddy H , Hosten, Eric C , Kaye, Perry , Watkins, Gareth M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194048 , vital:45418 , xlink:href="https://doi.org/10.1515/ncrs-2019-0698"
- Description: C11H8O4, monoclinic, P21/c (no. 14), a = 4.5947(2) Å, b = 10.5414(3) Å, c = 19.1611(7) Å, β = 94.084(2)°, V = 925.70(6) Å3, Z = 4, Rgt(F) = 0.0376, wRref(F 2) = 0.1109,T = 200(2) K.CCDC no.: 1906383
- Full Text:
- Date Issued: 2020
The crystal structure of 2-oxo-2H-chromen-4-yl acetate, C11H8O4
- Hulushe, Siya T, Manyeruke, Meloddy H, Hosten, Eric C, Kaye, Perry, Watkins, Gareth M, Krause, Rui W M
- Authors: Hulushe, Siya T , Manyeruke, Meloddy H , Hosten, Eric C , Kaye, Perry , Watkins, Gareth M , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193442 , vital:45332 , xlink:href="https://doi.org/10.1515/ncrs-2019-0698"
- Description: C11H8O4, monoclinic, P21/c (no. 14), a = 4.5947(2) Å, b = 10.5414(3) Å, c = 19.1611(7) Å, β = 94.084(2)°, V = 925.70(6) Å3, Z = 4, Rgt(F) = 0.0376, wRref(F 2) = 0.1109,T = 200(2) K.CCDC no.: 1906383
- Full Text:
- Date Issued: 2020
- Authors: Hulushe, Siya T , Manyeruke, Meloddy H , Hosten, Eric C , Kaye, Perry , Watkins, Gareth M , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193442 , vital:45332 , xlink:href="https://doi.org/10.1515/ncrs-2019-0698"
- Description: C11H8O4, monoclinic, P21/c (no. 14), a = 4.5947(2) Å, b = 10.5414(3) Å, c = 19.1611(7) Å, β = 94.084(2)°, V = 925.70(6) Å3, Z = 4, Rgt(F) = 0.0376, wRref(F 2) = 0.1109,T = 200(2) K.CCDC no.: 1906383
- Full Text:
- Date Issued: 2020
Rhodes University Graduation Ceremony 2012
- Authors: Rhodes University
- Date: 2012
- Language: English
- Type: text
- Identifier: vital:8135 , http://hdl.handle.net/10962/d1007245
- Description: Rhodes University Graduation Ceremonies 2012 [at] 1820 Settlers National Monument Thursday, 12 April at 18.00 [and] Friday, 13 April at 10:30; 14:30 & 18:00 [and] Saturday, 14 April at 10:30 , Rhodes University Awards, Scholarships, Bursaries and Prizes 2012
- Full Text:
- Date Issued: 2012
- Authors: Rhodes University
- Date: 2012
- Language: English
- Type: text
- Identifier: vital:8135 , http://hdl.handle.net/10962/d1007245
- Description: Rhodes University Graduation Ceremonies 2012 [at] 1820 Settlers National Monument Thursday, 12 April at 18.00 [and] Friday, 13 April at 10:30; 14:30 & 18:00 [and] Saturday, 14 April at 10:30 , Rhodes University Awards, Scholarships, Bursaries and Prizes 2012
- Full Text:
- Date Issued: 2012
Application of Baylis-Hillman methodology in the synthesis of HIV-1 enzyme inhibitors
- Authors: Manyeruke, Meloddy Hlatini
- Date: 2015
- Subjects: HIV infections , Enzyme inhibitors , AZT (Drug) , Bioconjugates
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4540 , http://hdl.handle.net/10962/d1017920
- Description: The application of Baylis-Hillman methodology has afforded access to a range of β-hydroxypropionate ester-AZT conjugates as potential dual-action HIV-1 IN/RT inhibitors. Two families comprising a total of nine β-hydroxypropionate ester-AZT conjugates were synthesised. The first family was accessed using O-benzylated salicylaldehydes and methyl acrylate and the second from unprotected salicylaldehydes using tert-butyl acrylate as the activated alkene. Spectroscopic methods were employed to fully characterize the compounds. Propargylation of the respective Baylis-Hillman adducts was achieved via conjugate addition of propargylamine. The resulting products were then employed in Cu(I)-catalysed “click” reactions with azidothymidine (AZT) to yield the desired β-hydroxypropionate ester-AZT conjugates. Exploratory studies were also conducted to access 4-hydroxycoumarins from Baylis-Hillman derived adducts and to construct customized chiral Baylis-Hillman reaction sites. Many 4- hydroxycoumarins are known to exhibit a wide range of biological activities, and extending Baylis-Hillman methodology to access these systems is an important challenge. Two approaches were investigated. The first involved the formation of a 4-phthalimidocoumarin, aromatisation and hydrolysis of which was expected to lead to the 4-hydroxycoumarin target. The second, a variation of the first, involved the use of 4-(chrolomethyl)coumarin intermediates. Unfortunately, while various intermediates were prepared and characterised, neither approach led ultimately to the desired targets. N-substituted borneol-10-sulfonamides were constructed from camphor-10- sulfonyl chloride as chiral Baylis-Hillman reaction sites. In a preliminary study, however, none of the N-substituted borneol-10-sulfonamides exhibited Baylis-Hillman catalytic activity.
- Full Text:
- Date Issued: 2015
- Authors: Manyeruke, Meloddy Hlatini
- Date: 2015
- Subjects: HIV infections , Enzyme inhibitors , AZT (Drug) , Bioconjugates
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4540 , http://hdl.handle.net/10962/d1017920
- Description: The application of Baylis-Hillman methodology has afforded access to a range of β-hydroxypropionate ester-AZT conjugates as potential dual-action HIV-1 IN/RT inhibitors. Two families comprising a total of nine β-hydroxypropionate ester-AZT conjugates were synthesised. The first family was accessed using O-benzylated salicylaldehydes and methyl acrylate and the second from unprotected salicylaldehydes using tert-butyl acrylate as the activated alkene. Spectroscopic methods were employed to fully characterize the compounds. Propargylation of the respective Baylis-Hillman adducts was achieved via conjugate addition of propargylamine. The resulting products were then employed in Cu(I)-catalysed “click” reactions with azidothymidine (AZT) to yield the desired β-hydroxypropionate ester-AZT conjugates. Exploratory studies were also conducted to access 4-hydroxycoumarins from Baylis-Hillman derived adducts and to construct customized chiral Baylis-Hillman reaction sites. Many 4- hydroxycoumarins are known to exhibit a wide range of biological activities, and extending Baylis-Hillman methodology to access these systems is an important challenge. Two approaches were investigated. The first involved the formation of a 4-phthalimidocoumarin, aromatisation and hydrolysis of which was expected to lead to the 4-hydroxycoumarin target. The second, a variation of the first, involved the use of 4-(chrolomethyl)coumarin intermediates. Unfortunately, while various intermediates were prepared and characterised, neither approach led ultimately to the desired targets. N-substituted borneol-10-sulfonamides were constructed from camphor-10- sulfonyl chloride as chiral Baylis-Hillman reaction sites. In a preliminary study, however, none of the N-substituted borneol-10-sulfonamides exhibited Baylis-Hillman catalytic activity.
- Full Text:
- Date Issued: 2015
Rhodes University Graduation Ceremony 2015
- Authors: Rhodes University
- Date: 2015
- Language: English
- Type: Text
- Identifier: vital:8149 , http://hdl.handle.net/10962/d1019888
- Description: Rhodes University Graduation Ceremonies 2015 [at] 1820 Settlers National Monument Thursday, 09 April at 10.00 & 17:00 [and] Friday, 10 April at 10:00; 14:30 & 18:00 [and] Saturday, 11 April at 10:00 , Rhodes University Awards, Scholarships,Bursaries and Prizes 2015
- Full Text:
- Date Issued: 2015
- Authors: Rhodes University
- Date: 2015
- Language: English
- Type: Text
- Identifier: vital:8149 , http://hdl.handle.net/10962/d1019888
- Description: Rhodes University Graduation Ceremonies 2015 [at] 1820 Settlers National Monument Thursday, 09 April at 10.00 & 17:00 [and] Friday, 10 April at 10:00; 14:30 & 18:00 [and] Saturday, 11 April at 10:00 , Rhodes University Awards, Scholarships,Bursaries and Prizes 2015
- Full Text:
- Date Issued: 2015
Nonlinear optical behavior of lanthanide phthalocyanines and their conjugates with a selection of nanomaterials
- Authors: Sekhosana, Kutloano Edward
- Date: 2017
- Language: English
- Type: Thesis , Doctoral , PhD
- Identifier: http://hdl.handle.net/10962/4580 , vital:20695
- Description: This thesis presents novel asymmetrical and symmetrical lanthanide phthalocyanines (Pcs) characterized using a number techniques including proton nuclear magnetic resonance, electron spin resonance, time correlated single photon counting, FTIR spectrometry, MALDI-TOF mass spectrometry, UV-Vis spectrometry, Raman spectroscopy and CHNS elemental analysis. The design of theses lanthanide Pcs takes the form of mononuclear, binuclear, trinuclear, bis- and tris(phthalocyanines). Nanomaterials such as zinc oxide nanoparticles (ZnO NPs), multi-walled carbon nanotubes (MWCNTs) and graphene oxide nanosheets (GONS) (oxidized and reduced) were employed for covalent linkage to mono- and binuclear phthalocyanines as conjugates. Transmission electron microscopy was used to characterize ZnO NPs, MWCNTs and GONS alone and when linked to lanthanide Pcs. Lanthanide Pcs alone and when linked to ZnO NPs, MWCNTs and GONS where embedded in polymers such as poly (methyl methacrylate) (PMMA), poly (bisphenol A carbonate) (PBC) and poly (acrylic acid) (PAA) for thin film preparation. The thickness of the thin films was determined by utilization of the knife edge attachment of the A Bruker D8 Discover X-ray diffraction (XRD). Optical limiting properties of lanthanide Pcs alone and as conjugates in solution and when incorporated into polymers were determined by employing a Z-scan technique. It emerged that low symmetry lanthanide Pcs (19, 20 and 21), the blue forms of bis(phthalocyanines) (only in solution; 24 and 28) as well as tris(phthalocyanines) (30 and 31) exhibit low limiting threshold (Ilim) values in solution and thin films (particularly PBC and PAA). The low limiting threshold values make these lanthanide Pcs reliable optical limiters.
- Full Text:
- Date Issued: 2017
- Authors: Sekhosana, Kutloano Edward
- Date: 2017
- Language: English
- Type: Thesis , Doctoral , PhD
- Identifier: http://hdl.handle.net/10962/4580 , vital:20695
- Description: This thesis presents novel asymmetrical and symmetrical lanthanide phthalocyanines (Pcs) characterized using a number techniques including proton nuclear magnetic resonance, electron spin resonance, time correlated single photon counting, FTIR spectrometry, MALDI-TOF mass spectrometry, UV-Vis spectrometry, Raman spectroscopy and CHNS elemental analysis. The design of theses lanthanide Pcs takes the form of mononuclear, binuclear, trinuclear, bis- and tris(phthalocyanines). Nanomaterials such as zinc oxide nanoparticles (ZnO NPs), multi-walled carbon nanotubes (MWCNTs) and graphene oxide nanosheets (GONS) (oxidized and reduced) were employed for covalent linkage to mono- and binuclear phthalocyanines as conjugates. Transmission electron microscopy was used to characterize ZnO NPs, MWCNTs and GONS alone and when linked to lanthanide Pcs. Lanthanide Pcs alone and when linked to ZnO NPs, MWCNTs and GONS where embedded in polymers such as poly (methyl methacrylate) (PMMA), poly (bisphenol A carbonate) (PBC) and poly (acrylic acid) (PAA) for thin film preparation. The thickness of the thin films was determined by utilization of the knife edge attachment of the A Bruker D8 Discover X-ray diffraction (XRD). Optical limiting properties of lanthanide Pcs alone and as conjugates in solution and when incorporated into polymers were determined by employing a Z-scan technique. It emerged that low symmetry lanthanide Pcs (19, 20 and 21), the blue forms of bis(phthalocyanines) (only in solution; 24 and 28) as well as tris(phthalocyanines) (30 and 31) exhibit low limiting threshold (Ilim) values in solution and thin films (particularly PBC and PAA). The low limiting threshold values make these lanthanide Pcs reliable optical limiters.
- Full Text:
- Date Issued: 2017
Evaluation of teachers perceptions towards the implementation of inclusive education in Quantile 3 schools: A case of four subdistrictsin the Eastern Cape
- Authors: Hlatini-Mpomane, N W
- Date: 2020-05
- Subjects: Inclusive education
- Language: English
- Type: Doctoral theses , text
- Identifier: http://hdl.handle.net/10353/21613 , vital:51710
- Description: This study investigated the perceptions of teachers on inclusive education. Four sub districts in Eastern Cape Province were purposively selected and used as a case study approach. These assisted the researcher to enter the world of teachers (by interviewing SMTs and Office-Based educators/Inclusive Education Specialists). The Inclusive Education Specialist and SMTs ideas, suggestion and recommendations on inclusive education classrooms implementation were explored deeply. The research paradigm which the study adopted was qualitative, which centres on understanding the subjective world of human experiences. The qualitative research approach was adopted whereby interviews, observations of learners and their documents analysis were used to collect data. The findings of the study revealed that the all-Inclusive Education District of the sub-districts is between 9 and 10 years of experience implementing inclusive education instead of 17 years as stipulated in the WP6. It emerged that the involvement of SMTs in monitoring the Individual Support Plan (ISPs) in Public Ordinary School (POS) is not prioritized. There is more emphasis and involvement in Full-Service Schools since 2015. The findings further revealed that the teachers find it difficult to implement ISPs due to overload and overcrowding more especially in POS. All learners were declared as benefiting more when individual teaching is done, which is rare due to overload and overcrowding in both Full Service Schools and Public Service Schools. The study recommends that they should be extensive policy evaluation processes that should be done to measure the effectiveness of the Inclusive Education Policy. The perceptions and experiences of teachers should be captured and be utilized when evaluating the policy. The latter will not be achieved in isolation by teachers only, but with collaboration from learners, parents, community members and the entire education department in the Eastern Cape in line with the Ecological Systems’ theory. , Thesis (PhD) -- Faculty of Education, 2020
- Full Text:
- Date Issued: 2020-05
- Authors: Hlatini-Mpomane, N W
- Date: 2020-05
- Subjects: Inclusive education
- Language: English
- Type: Doctoral theses , text
- Identifier: http://hdl.handle.net/10353/21613 , vital:51710
- Description: This study investigated the perceptions of teachers on inclusive education. Four sub districts in Eastern Cape Province were purposively selected and used as a case study approach. These assisted the researcher to enter the world of teachers (by interviewing SMTs and Office-Based educators/Inclusive Education Specialists). The Inclusive Education Specialist and SMTs ideas, suggestion and recommendations on inclusive education classrooms implementation were explored deeply. The research paradigm which the study adopted was qualitative, which centres on understanding the subjective world of human experiences. The qualitative research approach was adopted whereby interviews, observations of learners and their documents analysis were used to collect data. The findings of the study revealed that the all-Inclusive Education District of the sub-districts is between 9 and 10 years of experience implementing inclusive education instead of 17 years as stipulated in the WP6. It emerged that the involvement of SMTs in monitoring the Individual Support Plan (ISPs) in Public Ordinary School (POS) is not prioritized. There is more emphasis and involvement in Full-Service Schools since 2015. The findings further revealed that the teachers find it difficult to implement ISPs due to overload and overcrowding more especially in POS. All learners were declared as benefiting more when individual teaching is done, which is rare due to overload and overcrowding in both Full Service Schools and Public Service Schools. The study recommends that they should be extensive policy evaluation processes that should be done to measure the effectiveness of the Inclusive Education Policy. The perceptions and experiences of teachers should be captured and be utilized when evaluating the policy. The latter will not be achieved in isolation by teachers only, but with collaboration from learners, parents, community members and the entire education department in the Eastern Cape in line with the Ecological Systems’ theory. , Thesis (PhD) -- Faculty of Education, 2020
- Full Text:
- Date Issued: 2020-05
Synthesis and evaluation of the medicinal potential of novel 4-hydroxycoumarin derivatives
- Authors: Manyeruke, Meloddy Hlatini
- Date: 2022-04-08
- Subjects: Uncatalogued
- Language: English
- Type: Academic theses , Doctoral theses , text
- Identifier: http://hdl.handle.net/10962/164458 , vital:41120 , doi:10.21504/10962/164458
- Description: This research has focused on the synthesis and biological evaluation of a broad range of compounds characterised by the presence of the pharmacologically significant 4-hydroxycoumalin scaffold. The compounds were designed to contain additional pharmachophoric centres to enhance bioactivity and generate lead compounds with dualaction potential. The use of 4-hydroxycoumarin as the primary synthon enabled access to various series of 4-hydroxycoumarin conjugates, the reactive 3-position on the 4-hydroxycoumarin moiety being exploited for regioselective construction of the targeted compounds in several steps. Some of the reactants required in the construction of these compounds were specially synthesised and included propargyloxy benzaldehydes, benzyloxy benzaldehydes and 2,3-dihydroxysuccino-dihydride. Overall, eight different families of novel compounds were accessed, comprising conjugates of 4-hydroxycoumarin with bisethylidenesuccinohyrazide, trifluoroacetamide, amino, benzyloxyphenyl-iminoethyl, benzylidenehyrazinyl-thiazoyl, benzylidenehydrazonoethyl, propargyloxybenzylidenehydrazonoethyl and phenylacryloyl moieties using protocols that required minimal work-up and purification. The eighty novel compounds synthesised in the study were fully characterised using HMRS and advanced NMR techniques. Cytotoxicity, HIV-1 IN and PR inhibitory, and antitrypanosomal, antimalarial and anti-Mtb assays were conducted on the synthesised coumarin derivatives. Several compounds exhibited activity against HIV-1 IN, the most potent being a bis-ethylidenesuccinohyrazide with an IC50 value of 3.5 μM. Various compounds exhibited anti-malarial activity (% pLDH viability in the range 62-77%), anti-trypanosomal activity (the most potent with an IC50 = 0.9 μM against T.b. brucei) and a measure of anti-Mtb activity. Apart from two chalconyl derivatives, none of the synthesised compounds exhibited significant cytotoxicity. Conflicting results were obtained from the in silico docking studies; in some cases supporting the observed in vitro assay data while, in others, exhibiting no correlation. , Thesis (PhD) -- Faculty of Science, Chemistry, 2020
- Full Text:
- Date Issued: 2022-04-08
- Authors: Manyeruke, Meloddy Hlatini
- Date: 2022-04-08
- Subjects: Uncatalogued
- Language: English
- Type: Academic theses , Doctoral theses , text
- Identifier: http://hdl.handle.net/10962/164458 , vital:41120 , doi:10.21504/10962/164458
- Description: This research has focused on the synthesis and biological evaluation of a broad range of compounds characterised by the presence of the pharmacologically significant 4-hydroxycoumalin scaffold. The compounds were designed to contain additional pharmachophoric centres to enhance bioactivity and generate lead compounds with dualaction potential. The use of 4-hydroxycoumarin as the primary synthon enabled access to various series of 4-hydroxycoumarin conjugates, the reactive 3-position on the 4-hydroxycoumarin moiety being exploited for regioselective construction of the targeted compounds in several steps. Some of the reactants required in the construction of these compounds were specially synthesised and included propargyloxy benzaldehydes, benzyloxy benzaldehydes and 2,3-dihydroxysuccino-dihydride. Overall, eight different families of novel compounds were accessed, comprising conjugates of 4-hydroxycoumarin with bisethylidenesuccinohyrazide, trifluoroacetamide, amino, benzyloxyphenyl-iminoethyl, benzylidenehyrazinyl-thiazoyl, benzylidenehydrazonoethyl, propargyloxybenzylidenehydrazonoethyl and phenylacryloyl moieties using protocols that required minimal work-up and purification. The eighty novel compounds synthesised in the study were fully characterised using HMRS and advanced NMR techniques. Cytotoxicity, HIV-1 IN and PR inhibitory, and antitrypanosomal, antimalarial and anti-Mtb assays were conducted on the synthesised coumarin derivatives. Several compounds exhibited activity against HIV-1 IN, the most potent being a bis-ethylidenesuccinohyrazide with an IC50 value of 3.5 μM. Various compounds exhibited anti-malarial activity (% pLDH viability in the range 62-77%), anti-trypanosomal activity (the most potent with an IC50 = 0.9 μM against T.b. brucei) and a measure of anti-Mtb activity. Apart from two chalconyl derivatives, none of the synthesised compounds exhibited significant cytotoxicity. Conflicting results were obtained from the in silico docking studies; in some cases supporting the observed in vitro assay data while, in others, exhibiting no correlation. , Thesis (PhD) -- Faculty of Science, Chemistry, 2020
- Full Text:
- Date Issued: 2022-04-08
Challenges encountered by schools in the implementation of inclusive education in the Eastern Cape: a survey study in the Ngcobo District
- Hlatini-Mphomane, Nyameka Winnifred
- Authors: Hlatini-Mphomane, Nyameka Winnifred
- Date: 2013
- Subjects: Inclusive education -- Evaluation , Eastern Cape -- South Africa
- Language: English
- Type: Thesis , Masters , M Ed
- Identifier: vital:18441 , http://hdl.handle.net/11260/d1007258
- Description: This study investigated challenges encountered by schools in the implementation of inclusive education in the Eastern Cape. It was a Survey Study carried out in Ngcobo District. School principals of randomly-sampled mainstream schools and special schools participated in this research project. The key research question that the study sought to answer was: What are the challenges encountered by schools in the implementation of Inclusive Education in the Ngcobo District of the Eastern Cape Province? The following were the sub-research questions: (a). How does the lack of specialized or in-service, trained human resource personnel challenge or hinder the implementation of Inclusive Education? (b). How is the implementation of Inclusive Education affected by available infra-structure? (c). How do the attitudes of stake holders such as learners, educators (ILST) and parents (SGB) affect the implementation of inclusive education? The findings of the study revealed that: There is a gross shortage of educators qualified in inclusive education or related streams, and in some schools none at all. Institution Level Support Teams (ILSTs) in some schools have not been established and some of those that are established are not functional. Needed specialists such as psychologists and occupational therapists are not available in special schools. Workshops or in-service training for educators generally are held for to ILSTs only instead of all educators and SMTs. School buildings and toilets have not been adapted for when inclusion is to be implemented and there are no specific, funded departmental projects to rectify this. Assistive devices for learners experiencing barriers to teaching, learning and development are rarely found. There are no clear departmental budgets to ensure the policy is implemented in ordinary schools. Negative attitudes of some parents, teachers and learners toward inclusion still exist. The following recommendations were made for consideration in order to facilitate the smooth implementation of Inclusive Education in the schools. There should be adequate provision of human resource training and development Educators have to further their studies in Inclusive Education. There should be provision of a specific budget for buildings. Maintenance funds ought to be used to renovate school buildings so as to be Inclusive Education friendly. Advocacy and awareness programmes for different stakeholders should be conducted.
- Full Text:
- Date Issued: 2013
- Authors: Hlatini-Mphomane, Nyameka Winnifred
- Date: 2013
- Subjects: Inclusive education -- Evaluation , Eastern Cape -- South Africa
- Language: English
- Type: Thesis , Masters , M Ed
- Identifier: vital:18441 , http://hdl.handle.net/11260/d1007258
- Description: This study investigated challenges encountered by schools in the implementation of inclusive education in the Eastern Cape. It was a Survey Study carried out in Ngcobo District. School principals of randomly-sampled mainstream schools and special schools participated in this research project. The key research question that the study sought to answer was: What are the challenges encountered by schools in the implementation of Inclusive Education in the Ngcobo District of the Eastern Cape Province? The following were the sub-research questions: (a). How does the lack of specialized or in-service, trained human resource personnel challenge or hinder the implementation of Inclusive Education? (b). How is the implementation of Inclusive Education affected by available infra-structure? (c). How do the attitudes of stake holders such as learners, educators (ILST) and parents (SGB) affect the implementation of inclusive education? The findings of the study revealed that: There is a gross shortage of educators qualified in inclusive education or related streams, and in some schools none at all. Institution Level Support Teams (ILSTs) in some schools have not been established and some of those that are established are not functional. Needed specialists such as psychologists and occupational therapists are not available in special schools. Workshops or in-service training for educators generally are held for to ILSTs only instead of all educators and SMTs. School buildings and toilets have not been adapted for when inclusion is to be implemented and there are no specific, funded departmental projects to rectify this. Assistive devices for learners experiencing barriers to teaching, learning and development are rarely found. There are no clear departmental budgets to ensure the policy is implemented in ordinary schools. Negative attitudes of some parents, teachers and learners toward inclusion still exist. The following recommendations were made for consideration in order to facilitate the smooth implementation of Inclusive Education in the schools. There should be adequate provision of human resource training and development Educators have to further their studies in Inclusive Education. There should be provision of a specific budget for buildings. Maintenance funds ought to be used to renovate school buildings so as to be Inclusive Education friendly. Advocacy and awareness programmes for different stakeholders should be conducted.
- Full Text:
- Date Issued: 2013
Exploring intermolecular contacts in multi-substituted benzaldehyde derivatives: X-ray, Hirshfeld surface and lattice energy analyses
- Hulushe, Siya T, Manyeruke, Meloddy H, Louzada, Marcel, Rigin, Sergei, Hosten, Eric C, Watkins, Gareth M
- Authors: Hulushe, Siya T , Manyeruke, Meloddy H , Louzada, Marcel , Rigin, Sergei , Hosten, Eric C , Watkins, Gareth M
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/148483 , vital:38743 , DOI: 10.1039/C9RA10752E
- Description: Crystal structures of six benzaldehyde derivatives (1–6) have been determined and their supramolecular networks were established by an X-ray crystallographic study. The study has shown that the compounds are linked by various intermolecular interactions such as weak C–H⋯O hydrogen bonding, and C–H⋯π, π–π and halogen bonding interactions which consolidate and strengthen the formation of these molecular assemblies. The carbonyl group generates diverse synthons in 1–6 via intermolecular C–H⋯O hydrogen bonds. An interplay of C–H⋯O hydrogen bonds, and C–H⋯π and π–π stacking interactions facilitates the formation of multi-dimensional supramolecular networks. Crystal packings in 4 and 5 are further generated by type I halogen⋯halogen bonding interactions. The differences in crystal packing are represented by variation of substitution positions in the compounds. Structure 3 is isomorphous with 4 but there are subtle differences in their crystal packing.
- Full Text:
- Date Issued: 2020
- Authors: Hulushe, Siya T , Manyeruke, Meloddy H , Louzada, Marcel , Rigin, Sergei , Hosten, Eric C , Watkins, Gareth M
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/148483 , vital:38743 , DOI: 10.1039/C9RA10752E
- Description: Crystal structures of six benzaldehyde derivatives (1–6) have been determined and their supramolecular networks were established by an X-ray crystallographic study. The study has shown that the compounds are linked by various intermolecular interactions such as weak C–H⋯O hydrogen bonding, and C–H⋯π, π–π and halogen bonding interactions which consolidate and strengthen the formation of these molecular assemblies. The carbonyl group generates diverse synthons in 1–6 via intermolecular C–H⋯O hydrogen bonds. An interplay of C–H⋯O hydrogen bonds, and C–H⋯π and π–π stacking interactions facilitates the formation of multi-dimensional supramolecular networks. Crystal packings in 4 and 5 are further generated by type I halogen⋯halogen bonding interactions. The differences in crystal packing are represented by variation of substitution positions in the compounds. Structure 3 is isomorphous with 4 but there are subtle differences in their crystal packing.
- Full Text:
- Date Issued: 2020
Synthesis, characterisation and evaluation of benzoxaborole-based hybrids as antiplasmodial agents
- Authors: Gumbo, Maureen
- Date: 2017
- Subjects: Malaria Chemotherapy , Antimalarials , Boron compounds , Drug resistance , Plasmodium falciparum , Drug development
- Language: English
- Type: Master's theses , text
- Identifier: http://hdl.handle.net/10962/59193 , vital:27456
- Description: Malaria is a mosquito-borne disease, which continues to pose a threat to the entire humanity. About 40% of the world population is estimated to be at risk of infections by malaria. Despite efforts undertaken by scientific community, government entities and international organizations, malaria is still rampant. The major problem is drug resistance, where the Plasmodium spp have over the past decades developed drug resistance against available drugs. In order to counter this problem, novel antimalarial drugs that are efficacious and with novel mode of action are of great necessity. Benzoxaborole derivatives have been shown to exhibit promising antimalarial activity against Plasmodium falciparum strains. Previous studies reported on the compounds such as 6-(2- (alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles, which showed good antimalarial activity against both W7 and 3D7 strains without significant toxicity. On the other hand, chloroquine (CQ) and cinnamic acids have a wide variety of biological activity including antimalarial activity. Herein, a hybridisation strategy was employed to synthesise new CQ-benzoxaborole and cinnamoyl-benzoxaborole hybrids. CQ-Benzoxaborole 2.12a-c and cinnamoylbenzoxaborole 2.11a-g hydrid molecules were synthesised in low to good yields. Their structural identities were confirmed using conventional spectroscopic techniques (1H and 13C NMR, and mass spectrometry). CQ-benzoxaborole compounds, however, showed instability, and only 2.12b was used for in vitro biological assay and showed activity comparable to CQ. Furthermore, in vitro biological assay revealed that compounds 2.11a-g poorly inhibited the growth of P. falciparum parasites. Interestingly, these compounds, however, exhibited satisfactory activity against Trypanosoma brucei with IC50 = 0.052 μM for compound 2.11g. The cell cytotoxicity assay of all final compounds confirmed that all CQ-benzoxaborole 2.12b and cinnamoyl-benzoxaborole 2.11a-g hybrids were non-toxic against HeLa cell lines. However, efforts to further expand the structure-activity relationship (SAR) of CQbenzoxaborole by increasing the length of the linker with one extra carbon (Scheme 2.10) were not possible as an important precursor 6-formylbenzoxaborole 2.29 could not be synthesized in sufficient yields. , Thesis (MSc) -- Faculty of Faculty of Science, Chemistry, 2017
- Full Text:
- Date Issued: 2017
- Authors: Gumbo, Maureen
- Date: 2017
- Subjects: Malaria Chemotherapy , Antimalarials , Boron compounds , Drug resistance , Plasmodium falciparum , Drug development
- Language: English
- Type: Master's theses , text
- Identifier: http://hdl.handle.net/10962/59193 , vital:27456
- Description: Malaria is a mosquito-borne disease, which continues to pose a threat to the entire humanity. About 40% of the world population is estimated to be at risk of infections by malaria. Despite efforts undertaken by scientific community, government entities and international organizations, malaria is still rampant. The major problem is drug resistance, where the Plasmodium spp have over the past decades developed drug resistance against available drugs. In order to counter this problem, novel antimalarial drugs that are efficacious and with novel mode of action are of great necessity. Benzoxaborole derivatives have been shown to exhibit promising antimalarial activity against Plasmodium falciparum strains. Previous studies reported on the compounds such as 6-(2- (alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles, which showed good antimalarial activity against both W7 and 3D7 strains without significant toxicity. On the other hand, chloroquine (CQ) and cinnamic acids have a wide variety of biological activity including antimalarial activity. Herein, a hybridisation strategy was employed to synthesise new CQ-benzoxaborole and cinnamoyl-benzoxaborole hybrids. CQ-Benzoxaborole 2.12a-c and cinnamoylbenzoxaborole 2.11a-g hydrid molecules were synthesised in low to good yields. Their structural identities were confirmed using conventional spectroscopic techniques (1H and 13C NMR, and mass spectrometry). CQ-benzoxaborole compounds, however, showed instability, and only 2.12b was used for in vitro biological assay and showed activity comparable to CQ. Furthermore, in vitro biological assay revealed that compounds 2.11a-g poorly inhibited the growth of P. falciparum parasites. Interestingly, these compounds, however, exhibited satisfactory activity against Trypanosoma brucei with IC50 = 0.052 μM for compound 2.11g. The cell cytotoxicity assay of all final compounds confirmed that all CQ-benzoxaborole 2.12b and cinnamoyl-benzoxaborole 2.11a-g hybrids were non-toxic against HeLa cell lines. However, efforts to further expand the structure-activity relationship (SAR) of CQbenzoxaborole by increasing the length of the linker with one extra carbon (Scheme 2.10) were not possible as an important precursor 6-formylbenzoxaborole 2.29 could not be synthesized in sufficient yields. , Thesis (MSc) -- Faculty of Faculty of Science, Chemistry, 2017
- Full Text:
- Date Issued: 2017
Design, development and evaluation of novel lead compounds as HIV-1 enzyme inhibitors
- Authors: Sekgota, Khethobole Cassius
- Date: 2015
- Subjects: Enzyme inhibitors , Viruses -- Reproduction , HIV (Viruses)
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4546 , http://hdl.handle.net/10962/d1017926
- Description: This project has been concerned with the application of the Baylis-Hillman methodology to the synthesis of medicinally important diketo acid analogues (cinnamate ester-AZT conjugates and 3-hydroxy ester-AZT conjugates) as dual-action HIV-1 IN/RT inhibitors; and on exploratory studies in the preparation of 3-(amidomethyl)-(1H)-2-quinolones as PR inhibitors; and (1H)-2- quinolone-AZT conjugates as dual action IN/RT inhibitors. A series of Baylis-Hillman adducts has been prepared, typically in moderate to excellent yield, by reacting 2-nitrobenzaldehyde with methyl acrylate, ethyl acrylate and methyl vinyl ketone in the presence of 1,4- diazabicyclo[2.2.2]octane (DABCO). Subsequently, various transformations that include conjugate addition of primary and secondary amines to the α,ß-unsaturated moiety to obtain 2- (aminomethyl)-3-hydroxy-3-(2-nitrophenyl)propanoate derivatives, effective SN2´ substitution of the BH ß-hydroxy by a Vilsmeier-Haack in situ-generated chloride to afford Baylis-Hillman allyl chlorides, iron in acetic acid-catalyzed cyclisation to 3-acetoxymethyl-(1H)-2-quinolone derivatives were achieved. Thus, using the Baylis-Hillman methodology, two nuanced classes of diketo acid analogues were constructed. These involved conjugating appropriate propargylamine derivatives with AZT using the „click‟ reaction. In an exploratory study, the quinolone derivative, precisely 3-acetoxymethyl- (1H)-quinol-2-one, was transformed into 3-hydroxymethyl-(1H)-quinol-2-one using potassium carbonate in a mixture of methanol and water (1:1). Following successful hydrolysis, the resulting alcohol was transformed to the corresponding chloride, 3-chloromethyl-(1H)-quinol-2- one, using thionyl chloride. Subsequent nucleophilic substitution afforded 3-(aminomethyl)- (1H)-2-quinolone derivatives which were subsequently transformed to 3-(amidomethyl)-(1H)-2- quinolones; and 3-[(propargylamino)-methyl]-(1H)-quinol-2-one as precursors to quinolone- AZT derivatives. All compounds were characterized by NMR, IR, and where appropriate, high resolution MS
- Full Text:
- Date Issued: 2015
- Authors: Sekgota, Khethobole Cassius
- Date: 2015
- Subjects: Enzyme inhibitors , Viruses -- Reproduction , HIV (Viruses)
- Language: English
- Type: Thesis , Masters , MSc
- Identifier: vital:4546 , http://hdl.handle.net/10962/d1017926
- Description: This project has been concerned with the application of the Baylis-Hillman methodology to the synthesis of medicinally important diketo acid analogues (cinnamate ester-AZT conjugates and 3-hydroxy ester-AZT conjugates) as dual-action HIV-1 IN/RT inhibitors; and on exploratory studies in the preparation of 3-(amidomethyl)-(1H)-2-quinolones as PR inhibitors; and (1H)-2- quinolone-AZT conjugates as dual action IN/RT inhibitors. A series of Baylis-Hillman adducts has been prepared, typically in moderate to excellent yield, by reacting 2-nitrobenzaldehyde with methyl acrylate, ethyl acrylate and methyl vinyl ketone in the presence of 1,4- diazabicyclo[2.2.2]octane (DABCO). Subsequently, various transformations that include conjugate addition of primary and secondary amines to the α,ß-unsaturated moiety to obtain 2- (aminomethyl)-3-hydroxy-3-(2-nitrophenyl)propanoate derivatives, effective SN2´ substitution of the BH ß-hydroxy by a Vilsmeier-Haack in situ-generated chloride to afford Baylis-Hillman allyl chlorides, iron in acetic acid-catalyzed cyclisation to 3-acetoxymethyl-(1H)-2-quinolone derivatives were achieved. Thus, using the Baylis-Hillman methodology, two nuanced classes of diketo acid analogues were constructed. These involved conjugating appropriate propargylamine derivatives with AZT using the „click‟ reaction. In an exploratory study, the quinolone derivative, precisely 3-acetoxymethyl- (1H)-quinol-2-one, was transformed into 3-hydroxymethyl-(1H)-quinol-2-one using potassium carbonate in a mixture of methanol and water (1:1). Following successful hydrolysis, the resulting alcohol was transformed to the corresponding chloride, 3-chloromethyl-(1H)-quinol-2- one, using thionyl chloride. Subsequent nucleophilic substitution afforded 3-(aminomethyl)- (1H)-2-quinolone derivatives which were subsequently transformed to 3-(amidomethyl)-(1H)-2- quinolones; and 3-[(propargylamino)-methyl]-(1H)-quinol-2-one as precursors to quinolone- AZT derivatives. All compounds were characterized by NMR, IR, and where appropriate, high resolution MS
- Full Text:
- Date Issued: 2015
Synthesis and in vitro biological evaluation of 2,3-substituted quinoline derivatives
- Bokosi, Fostino Raphael Bentry
- Authors: Bokosi, Fostino Raphael Bentry
- Date: 2020
- Subjects: Quinoline , Malaria Chemotherapy , Tuberculosis Chemotherapy , African trypanosomiasis Chemotherapy
- Language: English
- Type: Master's theses , text
- Identifier: http://hdl.handle.net/10962/163193 , vital:41017
- Description: The urgent need for new systemic pharmacological entities prompted us to report a library of 2,3-substituted quinoline derivatives. Considering the ubiquity of quinoline-containing compounds in pharmacologically active small molecules, synthesized 2,3-substituted quinoline derivatives were in vitro biologically evaluated for their potential antitubercular, antimalarial and antitrypanosomal activities. Quinoline scaffold was achieved by the Vilsmeier-Haack methodology, affording synthetically useful chloro and formyl substituents on C-2 and C-3 respectively. These two substituents acted as handles in expanding the chemical space around the quinoline ring. Target compounds were synthesized in six to seven steps, employing conventional synthetic organic protocols adapted from various literature. The final compounds were accessed in moderate to good yields. The structural identity of each compound was confirmed by common spectroscopic techniques. Aryl quinoline carboxamide derivatives 3.113 – 3.126 were isolated as rotamers, hence, Variable-Temperature Nuclear Magnetic Resonance (VT-NMR) was employed in resolving 1H splitting. At elevated temperature (~328 K); N-methylene carbons were not visible on 13C NMR due to signal line broadening effects. The presence of these nuclei in such cases was, however, supported by 2-dimensional NMR and high-resolution MS data. Most of the compounds achieved in this study displayed promising antimalarial activity against chloroquine-sensitive 3D7 strain of Plasmodium falciparum compared to antitrypanosomal activity against Trypanosoma brucei brucei 427 strain. In particular, compounds 3.80 and 3.108 showed superior activity against chloroquine-sensitive 3D7 P. falciparum strain with IC50 values < 1 μM. More importantly, most of the compounds were non-toxic as determined by HeLa cells, indicating their selectivity towards the parasites. Exploring the space provided on the quinoline scaffold revealed that methoxy incorporation on C-2 is very critical in enhancing antimalarial activity of this class of quinoline compounds. The preliminary SAR of compounds 3.57 – 3.72 showed that compounds containing the 3-cinnamate exhibited enhanced antimalarial activity compared to 2 and 4-cinnamates. Finally, benzamide compounds 3.113 − 3.126 showed poor activity against Mycobacterium tuberculosis H37Rv strain with only compounds 3.113, 3.117 – 3.120 and 3.126 showing appreciable MIC90 values in the range of 40 – 85 μM. , Thesis (MSc) -- Faculty of Science, Chemistry, 2020
- Full Text:
- Date Issued: 2020
- Authors: Bokosi, Fostino Raphael Bentry
- Date: 2020
- Subjects: Quinoline , Malaria Chemotherapy , Tuberculosis Chemotherapy , African trypanosomiasis Chemotherapy
- Language: English
- Type: Master's theses , text
- Identifier: http://hdl.handle.net/10962/163193 , vital:41017
- Description: The urgent need for new systemic pharmacological entities prompted us to report a library of 2,3-substituted quinoline derivatives. Considering the ubiquity of quinoline-containing compounds in pharmacologically active small molecules, synthesized 2,3-substituted quinoline derivatives were in vitro biologically evaluated for their potential antitubercular, antimalarial and antitrypanosomal activities. Quinoline scaffold was achieved by the Vilsmeier-Haack methodology, affording synthetically useful chloro and formyl substituents on C-2 and C-3 respectively. These two substituents acted as handles in expanding the chemical space around the quinoline ring. Target compounds were synthesized in six to seven steps, employing conventional synthetic organic protocols adapted from various literature. The final compounds were accessed in moderate to good yields. The structural identity of each compound was confirmed by common spectroscopic techniques. Aryl quinoline carboxamide derivatives 3.113 – 3.126 were isolated as rotamers, hence, Variable-Temperature Nuclear Magnetic Resonance (VT-NMR) was employed in resolving 1H splitting. At elevated temperature (~328 K); N-methylene carbons were not visible on 13C NMR due to signal line broadening effects. The presence of these nuclei in such cases was, however, supported by 2-dimensional NMR and high-resolution MS data. Most of the compounds achieved in this study displayed promising antimalarial activity against chloroquine-sensitive 3D7 strain of Plasmodium falciparum compared to antitrypanosomal activity against Trypanosoma brucei brucei 427 strain. In particular, compounds 3.80 and 3.108 showed superior activity against chloroquine-sensitive 3D7 P. falciparum strain with IC50 values < 1 μM. More importantly, most of the compounds were non-toxic as determined by HeLa cells, indicating their selectivity towards the parasites. Exploring the space provided on the quinoline scaffold revealed that methoxy incorporation on C-2 is very critical in enhancing antimalarial activity of this class of quinoline compounds. The preliminary SAR of compounds 3.57 – 3.72 showed that compounds containing the 3-cinnamate exhibited enhanced antimalarial activity compared to 2 and 4-cinnamates. Finally, benzamide compounds 3.113 − 3.126 showed poor activity against Mycobacterium tuberculosis H37Rv strain with only compounds 3.113, 3.117 – 3.120 and 3.126 showing appreciable MIC90 values in the range of 40 – 85 μM. , Thesis (MSc) -- Faculty of Science, Chemistry, 2020
- Full Text:
- Date Issued: 2020
Rhodeo, Vol. 22, No. 16
- Date: 1968-08-22
- Subjects: Grahamstown -- Newspapers , Journalism, Students -- South Africa , Rhodes University -- Activate , Rhodes University -- Students , Student newspapers and periodicals -- South Africa
- Language: English
- Type: Text
- Identifier: vital:14590 , http://hdl.handle.net/10962/d1019462
- Description: Rhodeo is the Independent Student Newspaper of Rhodes University. Located in Grahamstown, Rhodeo was established in 1947, and renamed in 1994 as Activate. During apartheid Rhodeo became an active part of the struggle for freedom of expression as part of the now defunct South African Student Press Union. Currently Activate is committed to informing Rhodes University students, staff and community members about relevant issues, mainly on campus. These issues range from hard news to more creative journalism. While Activate acts as a news source, one of its main objectives it to be accessible as a training ground for student journalists. The newspaper is run entirely by the students and is published twice a term. Activate is a free newspaper which receives an annual grant from the Rhodes University Student Representative Council, however, majority of its revenue is generated through advertising.
- Full Text:
- Date Issued: 1968-08-22
- Date: 1968-08-22
- Subjects: Grahamstown -- Newspapers , Journalism, Students -- South Africa , Rhodes University -- Activate , Rhodes University -- Students , Student newspapers and periodicals -- South Africa
- Language: English
- Type: Text
- Identifier: vital:14590 , http://hdl.handle.net/10962/d1019462
- Description: Rhodeo is the Independent Student Newspaper of Rhodes University. Located in Grahamstown, Rhodeo was established in 1947, and renamed in 1994 as Activate. During apartheid Rhodeo became an active part of the struggle for freedom of expression as part of the now defunct South African Student Press Union. Currently Activate is committed to informing Rhodes University students, staff and community members about relevant issues, mainly on campus. These issues range from hard news to more creative journalism. While Activate acts as a news source, one of its main objectives it to be accessible as a training ground for student journalists. The newspaper is run entirely by the students and is published twice a term. Activate is a free newspaper which receives an annual grant from the Rhodes University Student Representative Council, however, majority of its revenue is generated through advertising.
- Full Text:
- Date Issued: 1968-08-22
Agreement and coordination in XiTsonga, SeSotho and IsiXhosa: an optimality theoretic perspective
- Authors: Mitchley, Hazel
- Date: 2016
- Language: English
- Type: Thesis , Masters , MA
- Identifier: http://hdl.handle.net/10962/3423 , vital:20491
- Description: This thesis provides a unified Optimality Theoretic analysis of subject-verb agreement with coordinated preverbal subjects in three Southern Bantu languages: Xitsonga (S53), Sesotho (S33), and isiXhosa (S41). This analysis is then used to formulate a typology of agreement resolution strategies and the contexts which trigger them. Although some accounts in the Bantu literature suggest that agreement with coordinate structures is avoided by speakers (e.g. Schadeberg 1992, Voeltz 1971) especially when conjuncts are from different noun classes, I show that there is ample evidence to the contrary, and that the subject marker used is dependent on several factors, including (i) the [-HUMAN] specification on the conjuncts, (ii) whether the conjuncts are singular or plural, (iii) whether or not the conjuncts both carry the same noun class feature, and (iv) the order of the conjuncts. This thesis shows that there are various agreement resolution strategies which can beused: 1) agreement with the [+HUMAN] feature on the conjuncts, 2) agreement with the[-HUMAN] feature on the conjuncts, 3) agreement with the noun class feature on both conjuncts, 4) agreement with the noun class feature on the conjunct closest to the verb, and 5) agreement with the noun class feature on the conjunct furthest from the verb. Not all of these strategies are used by all languages, nor are these strategies interchangeable in the languages which do use them – instead, multiple factors conspire to trigger the use of a specific agreement strategy within a specific agreement featural context. I show that these effects can be captured using Optimality Theory (Prince and Smolensky 2004). The analysis makes use of seven constraints: RES#, MAX[+H], MAX[-H], DEP[-H], MAXNC, DEPNC, and AGREECLOSEST. The hierarchical ranking of these constraints not only accounts for the confinement of particular strategies to specific agreement featural contexts within a language, but also accounts for the cross-linguistic differences in the use of these strategies. I end off by examining the typological implications which follow from the OT analysis provided in this thesis.
- Full Text:
- Date Issued: 2016
- Authors: Mitchley, Hazel
- Date: 2016
- Language: English
- Type: Thesis , Masters , MA
- Identifier: http://hdl.handle.net/10962/3423 , vital:20491
- Description: This thesis provides a unified Optimality Theoretic analysis of subject-verb agreement with coordinated preverbal subjects in three Southern Bantu languages: Xitsonga (S53), Sesotho (S33), and isiXhosa (S41). This analysis is then used to formulate a typology of agreement resolution strategies and the contexts which trigger them. Although some accounts in the Bantu literature suggest that agreement with coordinate structures is avoided by speakers (e.g. Schadeberg 1992, Voeltz 1971) especially when conjuncts are from different noun classes, I show that there is ample evidence to the contrary, and that the subject marker used is dependent on several factors, including (i) the [-HUMAN] specification on the conjuncts, (ii) whether the conjuncts are singular or plural, (iii) whether or not the conjuncts both carry the same noun class feature, and (iv) the order of the conjuncts. This thesis shows that there are various agreement resolution strategies which can beused: 1) agreement with the [+HUMAN] feature on the conjuncts, 2) agreement with the[-HUMAN] feature on the conjuncts, 3) agreement with the noun class feature on both conjuncts, 4) agreement with the noun class feature on the conjunct closest to the verb, and 5) agreement with the noun class feature on the conjunct furthest from the verb. Not all of these strategies are used by all languages, nor are these strategies interchangeable in the languages which do use them – instead, multiple factors conspire to trigger the use of a specific agreement strategy within a specific agreement featural context. I show that these effects can be captured using Optimality Theory (Prince and Smolensky 2004). The analysis makes use of seven constraints: RES#, MAX[+H], MAX[-H], DEP[-H], MAXNC, DEPNC, and AGREECLOSEST. The hierarchical ranking of these constraints not only accounts for the confinement of particular strategies to specific agreement featural contexts within a language, but also accounts for the cross-linguistic differences in the use of these strategies. I end off by examining the typological implications which follow from the OT analysis provided in this thesis.
- Full Text:
- Date Issued: 2016
(Re-)inventing our selves/ourselves : identity and community in contemporary South African short fiction cycles.
- Authors: Marais, Susan Jacqueline
- Date: 2014
- Subjects: South African fiction (English) -- History and criticism , Matlou, Joël -- Criticism and interpretation , Magona, Sindiwe -- Criticism and interpretation , Vladislavić, Ivan, 1957- -- Criticism and interpretation , Wicomb, Zoë -- Criticism and interpretation
- Language: English
- Type: Thesis , Doctoral , PhD
- Identifier: vital:2326 , http://hdl.handle.net/10962/d1016357
- Description: In this study I focus on a number of collections of short fiction by the South African writers Joël Matlou, Sindiwe Magona, Zoë Wicomb and Ivan Vladislavić, all of which evince certain of the characteristics of short story cycles or sequences. In other words, they display what Forrest L. Ingram describes as “a double tendency of asserting the individuality of [their] components on the one hand and of highlighting, on the other, the bonds of unity which make the many into a single whole”. The cycle form, thus defined, is characterised by a paradoxical yet productive and frequently unresolved tension between “the individuality of each of the stories and the necessities of the larger unit”, between “the one and the many”, and between cohesion and fragmentation. It is this “dynamic structure of connection and disconnection” which singularly equips the genre to represent the interrelationship of singular and collective identities, or the “coherent multiplicity of community”. Ingram, for example, asserts that “Numerous and varied connective strands draw the co-protagonists of any story cycle into a single community. … However this community may be achieved, it usually can be said to constitute the central character of a cycle”. Not unsurprisingly, then, in its dominant manifestations over much of the twentieth century the short story cycle demonstrated a marked inclination towards regionalism and the depiction of localised enclaves, and this tendency towards “place-based short story cycles” in which topographical unity is a conspicuous feature was as pronounced in South Africa as elsewhere. However, the specific collections which are my concern here increasingly employ innovative and self-reflexive narrative strategies that unsettle generic expectations and interrogate the notions of regionalism and community conventionally associated with the short story cycle. My investigation seeks to explain this shift in emphasis, and its particular significance within the South African context.
- Full Text:
- Date Issued: 2014
- Authors: Marais, Susan Jacqueline
- Date: 2014
- Subjects: South African fiction (English) -- History and criticism , Matlou, Joël -- Criticism and interpretation , Magona, Sindiwe -- Criticism and interpretation , Vladislavić, Ivan, 1957- -- Criticism and interpretation , Wicomb, Zoë -- Criticism and interpretation
- Language: English
- Type: Thesis , Doctoral , PhD
- Identifier: vital:2326 , http://hdl.handle.net/10962/d1016357
- Description: In this study I focus on a number of collections of short fiction by the South African writers Joël Matlou, Sindiwe Magona, Zoë Wicomb and Ivan Vladislavić, all of which evince certain of the characteristics of short story cycles or sequences. In other words, they display what Forrest L. Ingram describes as “a double tendency of asserting the individuality of [their] components on the one hand and of highlighting, on the other, the bonds of unity which make the many into a single whole”. The cycle form, thus defined, is characterised by a paradoxical yet productive and frequently unresolved tension between “the individuality of each of the stories and the necessities of the larger unit”, between “the one and the many”, and between cohesion and fragmentation. It is this “dynamic structure of connection and disconnection” which singularly equips the genre to represent the interrelationship of singular and collective identities, or the “coherent multiplicity of community”. Ingram, for example, asserts that “Numerous and varied connective strands draw the co-protagonists of any story cycle into a single community. … However this community may be achieved, it usually can be said to constitute the central character of a cycle”. Not unsurprisingly, then, in its dominant manifestations over much of the twentieth century the short story cycle demonstrated a marked inclination towards regionalism and the depiction of localised enclaves, and this tendency towards “place-based short story cycles” in which topographical unity is a conspicuous feature was as pronounced in South Africa as elsewhere. However, the specific collections which are my concern here increasingly employ innovative and self-reflexive narrative strategies that unsettle generic expectations and interrogate the notions of regionalism and community conventionally associated with the short story cycle. My investigation seeks to explain this shift in emphasis, and its particular significance within the South African context.
- Full Text:
- Date Issued: 2014
Rhodeo, Vol. 22, No. 17
- Date: 1968-08-29
- Subjects: Grahamstown -- Newspapers , Journalism, Students -- South Africa , Rhodes University -- Activate , Rhodes University -- Students , Student newspapers and periodicals -- South Africa
- Language: English
- Type: Text
- Identifier: vital:14591 , http://hdl.handle.net/10962/d1019463
- Description: Rhodeo is the Independent Student Newspaper of Rhodes University. Located in Grahamstown, Rhodeo was established in 1947, and renamed in 1994 as Activate. During apartheid Rhodeo became an active part of the struggle for freedom of expression as part of the now defunct South African Student Press Union. Currently Activate is committed to informing Rhodes University students, staff and community members about relevant issues, mainly on campus. These issues range from hard news to more creative journalism. While Activate acts as a news source, one of its main objectives it to be accessible as a training ground for student journalists. The newspaper is run entirely by the students and is published twice a term. Activate is a free newspaper which receives an annual grant from the Rhodes University Student Representative Council, however, majority of its revenue is generated through advertising.
- Full Text:
- Date Issued: 1968-08-29
- Date: 1968-08-29
- Subjects: Grahamstown -- Newspapers , Journalism, Students -- South Africa , Rhodes University -- Activate , Rhodes University -- Students , Student newspapers and periodicals -- South Africa
- Language: English
- Type: Text
- Identifier: vital:14591 , http://hdl.handle.net/10962/d1019463
- Description: Rhodeo is the Independent Student Newspaper of Rhodes University. Located in Grahamstown, Rhodeo was established in 1947, and renamed in 1994 as Activate. During apartheid Rhodeo became an active part of the struggle for freedom of expression as part of the now defunct South African Student Press Union. Currently Activate is committed to informing Rhodes University students, staff and community members about relevant issues, mainly on campus. These issues range from hard news to more creative journalism. While Activate acts as a news source, one of its main objectives it to be accessible as a training ground for student journalists. The newspaper is run entirely by the students and is published twice a term. Activate is a free newspaper which receives an annual grant from the Rhodes University Student Representative Council, however, majority of its revenue is generated through advertising.
- Full Text:
- Date Issued: 1968-08-29
Rhodeo, Vol. 22, No. 8
- Subjects: Grahamstown -- Newspapers , Journalism, Students -- South Africa , Rhodes University -- Activate , Rhodes University -- Students , Student newspapers and periodicals -- South Africa
- Language: English
- Type: Text
- Identifier: vital:14583 , http://hdl.handle.net/10962/d1019455
- Description: Rhodeo is the Independent Student Newspaper of Rhodes University. Located in Grahamstown, Rhodeo was established in 1947, and renamed in 1994 as Activate. During apartheid Rhodeo became an active part of the struggle for freedom of expression as part of the now defunct South African Student Press Union. Currently Activate is committed to informing Rhodes University students, staff and community members about relevant issues, mainly on campus. These issues range from hard news to more creative journalism. While Activate acts as a news source, one of its main objectives it to be accessible as a training ground for student journalists. The newspaper is run entirely by the students and is published twice a term. Activate is a free newspaper which receives an annual grant from the Rhodes University Student Representative Council, however, majority of its revenue is generated through advertising.
- Full Text:
- Subjects: Grahamstown -- Newspapers , Journalism, Students -- South Africa , Rhodes University -- Activate , Rhodes University -- Students , Student newspapers and periodicals -- South Africa
- Language: English
- Type: Text
- Identifier: vital:14583 , http://hdl.handle.net/10962/d1019455
- Description: Rhodeo is the Independent Student Newspaper of Rhodes University. Located in Grahamstown, Rhodeo was established in 1947, and renamed in 1994 as Activate. During apartheid Rhodeo became an active part of the struggle for freedom of expression as part of the now defunct South African Student Press Union. Currently Activate is committed to informing Rhodes University students, staff and community members about relevant issues, mainly on campus. These issues range from hard news to more creative journalism. While Activate acts as a news source, one of its main objectives it to be accessible as a training ground for student journalists. The newspaper is run entirely by the students and is published twice a term. Activate is a free newspaper which receives an annual grant from the Rhodes University Student Representative Council, however, majority of its revenue is generated through advertising.
- Full Text: