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

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

doi:10.1039/d0md00277a

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

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

Medicinal Chemistry

Research output: Contribution to journal › Article › Research › peer-review

3 Citations (Scopus)

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.

Original language	English
Pages (from-to)	1413-1422
Number of pages	10
Journal	RSC Medicinal Chemistry
Volume	11
Issue number	12
DOIs	https://doi.org/10.1039/d0md00277a
Publication status	Published - 1 Dec 2020

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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. ",

author = "Brown, {Ronald W.} and Abdel-Megeed, {Ashraf M.} and Keller, {Paul A.} and Jones, {Amy J.} and Sykes, {Melissa L.} and Marcel Kaiser and Baell, {Jonathan B.} and Avery, {Vicky M.} and Hyland, {Christopher J.T.}",

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T1 - Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness

AU - Brown, Ronald W.

AU - Abdel-Megeed, Ashraf M.

AU - Keller, Paul A.

AU - Jones, Amy J.

AU - Sykes, Melissa L.

AU - Kaiser, Marcel

AU - Baell, Jonathan B.

AU - Avery, Vicky M.

AU - Hyland, Christopher J.T.

PY - 2020/12/1

Y1 - 2020/12/1

N2 - 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.

AB - 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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U2 - 10.1039/d0md00277a

DO - 10.1039/d0md00277a

M3 - Article

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JO - RSC Medicinal Chemistry

JF - RSC Medicinal Chemistry

IS - 12

ER -

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

Abstract

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