Design, Synthesis and Antitrypanosomal Activities of 2,6-Disubstituted-4,5,7-Trifluorobenzothiophenes

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.

Description

Keywords

Benzothiophenes, Fluorinated drugs, Antitrypanosomal activity, Sleeping sickness, Human African trypanosomiasis

Citation

Bhambra, A.S., Edgar, M., Elsegood, M.R.J. et al. (2016) Design, Synthesis and Antitrypanosomal Activities of 2,6-Disubstituted-4,5,7-Trifluorobenzothiophenes. European Journal of Medicinal Chemistry, online first

Rights

Research Institute

Institute for Allied Health Sciences Research
Leicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)