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

Journal Article


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. This journal is

Publication Date


  • 2020

Citation


  • Brown, R. W., Abdel-Megeed, A. M., Keller, P. A., Jones, A. J., Sykes, M. L., Kaiser, M., . . . Hyland, C. J. T. (2020). Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness. RSC Medicinal Chemistry, 11(12), 1413-1422. doi:10.1039/d0md00277a

Scopus Eid


  • 2-s2.0-85098117851

Start Page


  • 1413

End Page


  • 1422

Volume


  • 11

Issue


  • 12

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. This journal is

Publication Date


  • 2020

Citation


  • Brown, R. W., Abdel-Megeed, A. M., Keller, P. A., Jones, A. J., Sykes, M. L., Kaiser, M., . . . Hyland, C. J. T. (2020). Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness. RSC Medicinal Chemistry, 11(12), 1413-1422. doi:10.1039/d0md00277a

Scopus Eid


  • 2-s2.0-85098117851

Start Page


  • 1413

End Page


  • 1422

Volume


  • 11

Issue


  • 12