Application of the Morita-Baylis-Hillman reaction in the synthesis of 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones as potential HIV-1 integrase inhibitors
- Sekgota, Khethobole C, Majumder, Swarup, Isaacs, Michelle, Mnkandhla, Dumisani, Hoppe, Heinrich C, Khanye, Setshaba D, Kriel, Frederik H, Coates, Judy, Kaye, Perry T
- Authors: Sekgota, Khethobole C , Majumder, Swarup , Isaacs, Michelle , Mnkandhla, Dumisani , Hoppe, Heinrich C , Khanye, Setshaba D , Kriel, Frederik H , Coates, Judy , Kaye, Perry T
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/66178 , vital:28913 , https://doi.org/10.1016/j.bioorg.2017.09.015
- Description: publisher version , A practicable six-step synthetic pathway has been developed to access a library of novel 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones using Morita-Baylis-Hillman methodology. These compounds and their 3-[(N-cycloalkylamino)methyl]-2-quinolone precursors have been screened as potential HIV-1 integrase (IN) inhibitors. A concomitant survey of their activity against HIV-1 protease and reverse-transcriptase reveals selective inhibition of HIV-1 IN.
- Full Text: false
- Date Issued: 2017
- Authors: Sekgota, Khethobole C , Majumder, Swarup , Isaacs, Michelle , Mnkandhla, Dumisani , Hoppe, Heinrich C , Khanye, Setshaba D , Kriel, Frederik H , Coates, Judy , Kaye, Perry T
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/66178 , vital:28913 , https://doi.org/10.1016/j.bioorg.2017.09.015
- Description: publisher version , A practicable six-step synthetic pathway has been developed to access a library of novel 3-[(N-cycloalkylbenzamido)methyl]-2-quinolones using Morita-Baylis-Hillman methodology. These compounds and their 3-[(N-cycloalkylamino)methyl]-2-quinolone precursors have been screened as potential HIV-1 integrase (IN) inhibitors. A concomitant survey of their activity against HIV-1 protease and reverse-transcriptase reveals selective inhibition of HIV-1 IN.
- Full Text: false
- Date Issued: 2017
Factors influencing the shape of CW-OSL signal obtained by stimulation of very deep traps in carbon-doped aluminium oxide: an experimental study
- Nyirenda, Angel N, Chithambo, Makaiko L
- Authors: Nyirenda, Angel N , Chithambo, Makaiko L
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/115493 , vital:34149 , https://doi.org/10.1016/j.jlumin.2017.07.016
- Description: The optically stimulated luminescence from carbon-doped aluminium oxide (α-Al2O3:C) displays a peak with time under certain measurement conditions. In this paper, we present factors that influence the peak-like shape of continuous-wave optically stimulated luminescence (CW-OSL) signal. The report is based on the experimental study of OSL signals obtained by stimulation of very deep traps in α-Al2O3:C. Methods exploiting post-irradiation annealing, variable dose and temperature dependent OSL measurements were used in the investigation. It is found that the rising part of the CW-OSL peak is obtained when the rate of retrapping at the most optically active trap (main trap) exceeds the rate of direct radiative recombination following optical release of charges from all optically active traps. This is possible if, during optical stimulation, the primary trap responsible for OSL i.e. the main trap, is substantially unoccupied and the very deep, donor traps are substantially filled up. The rate of charge retrapping itself is deduced to depend on the occupancy of the acceptor traps i.e. shallow, main and secondary traps; concentration of charge carriers in the very deep, donor traps; the post-irradiation annealing temperature and the temperature at which the OSL is measured.
- Full Text: false
- Date Issued: 2017
- Authors: Nyirenda, Angel N , Chithambo, Makaiko L
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/115493 , vital:34149 , https://doi.org/10.1016/j.jlumin.2017.07.016
- Description: The optically stimulated luminescence from carbon-doped aluminium oxide (α-Al2O3:C) displays a peak with time under certain measurement conditions. In this paper, we present factors that influence the peak-like shape of continuous-wave optically stimulated luminescence (CW-OSL) signal. The report is based on the experimental study of OSL signals obtained by stimulation of very deep traps in α-Al2O3:C. Methods exploiting post-irradiation annealing, variable dose and temperature dependent OSL measurements were used in the investigation. It is found that the rising part of the CW-OSL peak is obtained when the rate of retrapping at the most optically active trap (main trap) exceeds the rate of direct radiative recombination following optical release of charges from all optically active traps. This is possible if, during optical stimulation, the primary trap responsible for OSL i.e. the main trap, is substantially unoccupied and the very deep, donor traps are substantially filled up. The rate of charge retrapping itself is deduced to depend on the occupancy of the acceptor traps i.e. shallow, main and secondary traps; concentration of charge carriers in the very deep, donor traps; the post-irradiation annealing temperature and the temperature at which the OSL is measured.
- Full Text: false
- Date Issued: 2017
Structural and optical properties of sol-gel derived α-Fe2O3 nanoparticles
- Mathevula, Langutani E, Noto, L L, Mothudi, Bakang M, Chithambo, Makaiko L, Dhlamini, M S
- Authors: Mathevula, Langutani E , Noto, L L , Mothudi, Bakang M , Chithambo, Makaiko L , Dhlamini, M S
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/115467 , vital:34145 , DOI: 10.1016/j.jlumin.2017.07.055
- Description: α-Fe2O3 nanoparticles of crystallite size between 3.9 and 9.5 nm were synthesized by a simple sol-gel method using iron (III) nitrate nonahydrate (Fe(NO3)3·9H2O) as a precursor. Polyvinyl alcohol (PVA) was added as a capping agent to avoid agglomeration of the nanoparticles. A single pure phase was obtained when the sample was annealed at 300 °C and 600 °C. The purity was further confirmed with the Fourier Transform Infrared Spectroscopy. The energy band gap of the materials was extrapolated from the Kubelka-Munk relation and it ranges between 1.8 and 2.3 eV. The Photoluminescence of the 3 samples shows a broad emission spectrum centered at about 422 nm when excited by a 336 nm lamp. The emission peaks intensities increased with an increase in the annealing temperature, accept for the 576 nm peak, which was quenched as the temperature increased from 300 °C to 600 °C. The thermoluminescence glow curves were carried out at different heating rates and the samples were exposed to different beta particle doses (82–1315 Gy). The activation energy of the trapped electrons was determined.
- Full Text: false
- Date Issued: 2017
- Authors: Mathevula, Langutani E , Noto, L L , Mothudi, Bakang M , Chithambo, Makaiko L , Dhlamini, M S
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/115467 , vital:34145 , DOI: 10.1016/j.jlumin.2017.07.055
- Description: α-Fe2O3 nanoparticles of crystallite size between 3.9 and 9.5 nm were synthesized by a simple sol-gel method using iron (III) nitrate nonahydrate (Fe(NO3)3·9H2O) as a precursor. Polyvinyl alcohol (PVA) was added as a capping agent to avoid agglomeration of the nanoparticles. A single pure phase was obtained when the sample was annealed at 300 °C and 600 °C. The purity was further confirmed with the Fourier Transform Infrared Spectroscopy. The energy band gap of the materials was extrapolated from the Kubelka-Munk relation and it ranges between 1.8 and 2.3 eV. The Photoluminescence of the 3 samples shows a broad emission spectrum centered at about 422 nm when excited by a 336 nm lamp. The emission peaks intensities increased with an increase in the annealing temperature, accept for the 576 nm peak, which was quenched as the temperature increased from 300 °C to 600 °C. The thermoluminescence glow curves were carried out at different heating rates and the samples were exposed to different beta particle doses (82–1315 Gy). The activation energy of the trapped electrons was determined.
- Full Text: false
- Date Issued: 2017
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