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

Basic Information

ID: ALA3751823

Journal: Eur J Med Chem

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

Authors: Bhambra AS, Edgar M, Elsegood MR, Li Y, Weaver GW, Arroo RR, Yardley V, Burrell-Saward H, Krystof V.

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.

CiteXplore: 26698538

DOI: 10.1016/j.ejmech.2015.11.043

Patent ID: ┄