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Investigation of thiazolyl–benzothiophenamides as potential agents for African sleeping sickness

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Abstract

African sleeping sickness is a potentially fatal neglected disease affecting sub-Saharan Africa. High-throughput screening identified the thiazolyl–benzothiophenamide 1 to be active against the causative parasite, Trypanosoma brucei. This work establishes structure–activity relationships of 1, guiding the design of second generation derivatives. After screening against the clinically relevant species T. b. rhodesiense, the derivative 16 was identified as a suitable candidate for further investigation.

Graphical abstract: Investigation of thiazolyl–benzothiophenamides as potential agents for African sleeping sickness

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Submitted
04 Aug 2020
Accepted
10 Sep 2020
First published
23 Sep 2020

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

Investigation of thiazolyl–benzothiophenamides as potential agents for African sleeping sickness

R. W. Brown, A. M. Abdel-Megeed, P. A. Keller, A. J. Jones, M. L. Sykes, M. Kaiser, J. B. Baell, V. M. Avery and C. J. T. Hyland, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/D0MD00277A

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