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Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness.

Ronald W BrownAshraf M Abdel-MegeedPaul A KellerAmy J JonesMelissa Louise SykesMarcel KaiserJonathan B BaellVicky Marie AveryChristopher J T Hyland
Published in: RSC medicinal chemistry (2020)
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.
Keyphrases
  • plasmodium falciparum
  • human health
  • toxoplasma gondii