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  • Title: Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes.
    Author: Bhambra AS, Edgar M, Elsegood MRJ, Li Y, Weaver GW, Arroo RRJ, Yardley V, Burrell-Saward H, Krystof V.
    Journal: Eur J Med Chem; 2016 Jan 27; 108():347-353. PubMed ID: 26698538.
    Abstract:
    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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