Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes.

Avninder S Bhambra; Mark Edgar; Mark RJ Elsegood; Yuqi Li; George W Weaver; Randolph RJ Arroo; Vanessa Yardley; Hollie Burrell-Saward; Vladimir Krystof; (2015) Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes. European journal of medicinal chemistry, 108. pp. 347-353. ISSN 0223-5234 DOI: 10.1016/j.ejmech.2015.11.043
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Current treatments for Human African Trypanosomiasis (HAT) are limited in their application, have undesirable dosing regimens and unsatisfactory toxicities highlighting the need for the development of a safer drug pipeline. Our medicinal chemistry programme in developing rapidly accessible and modifiable heterocyclic scaffolds led to the design and synthesis of novel substituted benzothiophenes, with 6-benzimidazol-1-ylbenzothiophene derivatives demonstrating significant antitrypanosomal activities (IC50 < 1 μM) against Trypanosoma brucei rhodesiense and no toxicity towards mammalian cells.

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