- 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
- 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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Collections
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
SDG 03. Good Health and Well-Being
RU Department of Biochemistry, Microbiology and Bioinformatics
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