Expanding the SAR of Nontoxic Antiplasmodial Indolyl-3-ethanone Ethers and Thioethers:

Lunga, Mayibongwe J; Chisango, Ruramai L; Weyers, Carli; Isaacs, Michelle; Taylor, Dale; Edkins, Adrienne L; Khanye, Setshaba D; Hoppe, Heinrich C; Veale, Clinton G L

Title: Expanding the SAR of Nontoxic Antiplasmodial Indolyl-3-ethanone Ethers and Thioethers:
Creator: Lunga, Mayibongwe J
Creator: Chisango, Ruramai L
Creator: Weyers, Carli
Creator: Isaacs, Michelle
Creator: Taylor, Dale
Creator: Edkins, Adrienne L
Creator: Khanye, Setshaba D
Creator: Hoppe, Heinrich C
Creator: Veale, Clinton G L
Date Issued: 2018
Date: 2018
Type: text
Type: article
Identifier: http://hdl.handle.net/10962/164389
Identifier: vital:41114
Identifier: DOI: 10.1002/cmdc.201800235
Description: Despite major strides in reducing Plasmodium falciparum infections, this parasite still accounts for roughly half a million annual deaths. This problem is compounded by the decreased efficacy of artemisinin combination therapies. Therefore, the development and optimisation of novel antimalarial chemotypes is critical. In this study, we describe our strategic approach to optimise a class of previously reported antimalarials, resulting in the discovery of 1-(5-chloro-1H-indol-3-yl)-2-[(4-cyanophenyl)thio]ethanone (13) and 1-(5-chloro-1H-indol-3-yl)-2-[(4-nitrophenyl)thio]ethanone (14), whose activity was equipotent to that of chloroquine against the P. falciparum 3D7 strain.
Format: 10 pages
Format: pdf
Language: English
Relation: ChemMedChem
Relation: Lunga, M.J., Chisango, R.L., Weyers, C., Isaacs, M., Taylor, D., Edkins, A.L., Khanye, S.D., Hoppe, H.C. and Veale, C.G., 2018. Expanding the SAR of Nontoxic Antiplasmodial Indolyl-3-ethanone Ethers and Thioethers. ChemMedChem, 13(13), pp.1353-1362
Relation: ChemMedChem volume 13 number 13 1353 1362 May 2018 1860-7187
Rights: Publisher
Rights: Use of this resource is governed by the terms and conditions of the Wiley Library Online Terms of Use Statement (https://onlinelibrary.wiley.com/terms-and-conditions)

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RU DST/NRF SARChI for Molecular and Cellular Biology of the Eukaryotic Stress Response

Edkins, Adrienne Lesley (Associate Prof)

Veale, Clinton G L (Dr)

Khanye, David Setshaba (Associate Prof)

Hoppe, Heinrich C (Prof)

Isaacs, Michelle (Mrs)

RU Department of Chemistry

RU Department of Pharmacy

RU Department of Biochemistry, Microbiology and Bioinformatics

SDG 03. Good Health and Well-Being

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