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

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 , gui...

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Bibliographic Details
Published in:MedChemComm 2020-12, Vol.11 (12), p.1413-1422
Main Authors: Brown, Ronald W, Abdel-Megeed, Ashraf M, Keller, Paul A, Jones, Amy J, Sykes, Melissa L, Kaiser, Marcel, Baell, Jonathan B, Avery, Vicky M, Hyland, Christopher J. T
Format: Article
Language:English
Subjects:
African trypanosomiasis
Chemistry
High-throughput screening
Parasites
Screening
Vector-borne diseases
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Summary: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. African sleeping sickness is a potentially fatal neglected disease affecting sub-Saharan Africa.
ISSN:2632-8682
2040-2503
2632-8682
2040-2511
DOI:10.1039/d0md00277a