Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-Trifluorobenzothiophenes
journal contributionposted on 11.12.2015, 14:09 by Avninder S. Bhambra, Mark EdgarMark Edgar, Mark ElsegoodMark Elsegood, Yuqi Li, George WeaverGeorge Weaver, Randolph R.J. Arroo, Vanessa Yardley, Hollie Burrell-Saward, Vladimir Krystof
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.
This paper was supported by the Ministry of Education, Youth and Sports of the Czech Republic via the National Program of Sustainability I (grant LO1204), Loughborough University and De Montfort University.