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

0459007 - ÚEB 2017 RIV FR eng J - Journal Article
Bhambra, A.S. - Edgar, M. - Elsegood, M.R.J. - Li, Y. - Weaver, G.W. - Arroo, R.R.J. - Yardley, V. - Burrell-Saward, H. - Kryštof, Vladimír
Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes.
European Journal of Medicinal Chemistry. Roč. 108, JAN 27 (2016), s. 347-353. ISSN 0223-5234. E-ISSN 1768-3254
R&D Projects: GA MŠMT(CZ) LO1204
Institutional support: RVO:61389030
Keywords : Benzothiophenes * Fluorinated drugs * Antitrypanosomal activity
Subject RIV: EB - Genetics ; Molecular Biology
Impact factor: 4.519, year: 2016

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 mu M) against Trypanosoma brucei rhodesiense and no toxicity towards mammalian cells.
Permanent Link: http://hdl.handle.net/11104/0259204