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

RSC medicinal chemistry (2021-06-08)
Ronald W Brown, Ashraf M Abdel-Megeed, Paul A Keller, Amy J Jones, Melissa L Sykes, Marcel Kaiser, Jonathan B Baell, Vicky M Avery, Christopher J T Hyland
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Podophyllotoxin