Synthesis, antiplasmodial and antitrypanosomal evaluation of a series of novel 2-oxoquinoline-based thiosemicarbazone derivatives

Darrell, Oliver T; Hulushe, Siyabonga T; Mtshare, Thanduxolo Elihle; Beteck, Richard M; Isaacs, Michelle; Laming, Dustin; Khanye, Setshaba D; Hoppe, Heinrich C; Krause, Rui W M

Title: Synthesis, antiplasmodial and antitrypanosomal evaluation of a series of novel 2-oxoquinoline-based thiosemicarbazone derivatives
Creator: Darrell, Oliver T
Creator: Hulushe, Siyabonga T
Creator: Mtshare, Thanduxolo Elihle
Creator: Beteck, Richard M
Creator: Isaacs, Michelle
Creator: Laming, Dustin
Creator: Khanye, Setshaba D
Creator: Hoppe, Heinrich C
Creator: Krause, Rui W M
Date Issued: 2018
Date: 2018
Type: text
Type: article
Identifier: http://hdl.handle.net/10962/123117
Identifier: vital:35407
Identifier: https://doi.org/10.17159/0379-4350/2018/v71a25
Description: Herein a series of novel thiosemicarbazones (TSCs) derived from 2-oxoquinoline scaffold is reported, and the target compounds have been successfully synthesized and characterized using standard spectroscopic techniques. The in vitro biological activities of synthesized molecules were evaluated against Plasmodium falciparum malaria parasites (strain 3D7), Trypanosoma brucei brucei parasites (strain 427) and HeLa cells. All the compounds displayed modest or no activity at a concentration of 20 μM and percentage viability of >50 % was often observed. Except for compound 9o, none of the final compounds exhibited cytotoxic effects against HeLa cells at 20 μM.
Format: 8 pages
Format: pdf
Language: English
Relation: South African Journal of Chemistry
Relation: Darrell, O.T., Hulushe, S.T., Mtshare, T.E., Beteck, R.M., Isaacs, M., Laming, D., Hoppe, H.C., Krause, R.W. and Khanye, S.D., 2018. Synthesis, antiplasmodial and antitrypanosomal evaluation of a series of novel 2-oxoquinoline-based thiosemicarbazone derivatives. South African Journal of Chemistry, 71(1), pp.174-181.
Relation: South African Journal of Chemistry number 71 174 181 March 2018 1996-840X
Rights: South African Journal of Chemistry
Rights: Use of this resource is governed by the terms and conditions of the South African Journal of Chemistry Open Access Statement (http://www.scielo.org.za/revistas/sajc/iaboutj.htm)

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Khanye, David Setshaba (Associate Prof)

Krause, Rui Werner Maçedo (Prof)

RU Centre for Chemico- and Biomedicinal Research (CCBR)

Hoppe, Heinrich C (Prof)

Isaacs, Michelle (Mrs)

RU Department of Pharmacy

SDG 03. Good Health and Well-Being

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