Design, Synthesis and Antitrypanosomal Activities of 2,6-Disubstituted-4,5,7-Trifluorobenzothiophenes
Date
2015-11-30
Advisors
Journal Title
Journal ISSN
ISSN
Volume Title
Publisher
Elsevier
Type
Article
Peer reviewed
Yes
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