2. Academic Validation
  3. Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness

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

  • RSC Med Chem. 2020 Sep 23;11(12):1413-1422. doi: 10.1039/d0md00277a.
Ronald W Brown 1,  Ashraf M Abdel-Megeed 1,  Paul A Keller 1,  Amy J Jones 2,  Melissa L Sykes 2,  Marcel Kaiser 3 4,  Jonathan B Baell 5,  Vicky M Avery 2,  Christopher J T Hyland 1
Affiliations

Affiliations

  • 1 School of Chemistry and Molecular Bioscience, and Molecular Horizons Research Institute, University of Wollongong Wollongong 2522 NSW Australia chrhyl@uow.edu.au.
  • 2 Discovery Biology, Griffith Institute for Drug Discovery, Griffith University Brisbane Innovation Park Nathan 4111 Australia.
  • 3 Swiss Tropical and Public Health Institute Basel 4051 Switzerland.
  • 4 University of Basel 4003 Basel Switzerland.
  • 5 Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University Parkville 3052 Australia.
PMID: 34095848 DOI: 10.1039/d0md00277a
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.

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