AB 23-11-15 Manuscript[2].pdf (356.55 kB)

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

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journal contribution
posted on 11.12.2015 by Avninder S. Bhambra, Mark Edgar, Mark Elsegood, Yuqi Li, George 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.

Funding

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.

History

School

  • Science

Department

  • Chemistry

Published in

European Journal of Medicinal Chemistry

Citation

BHAMBRA, A.S. ...et al., 2016. Design, Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-Trifluorobenzothiophenes. European Journal of Medicinal Chemistry, 108, pp.347-353.

Publisher

© Elsevier

Version

AM (Accepted Manuscript)

Publisher statement

This work is made available according to the conditions of the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0) licence. Full details of this licence are available at: https://creativecommons.org/licenses/by-nc-nd/4.0/

Publication date

2016

Notes

This paper was accepted for publication in the journal European Journal of Medicinal Chemistry and the definitive published version is available at http://dx.doi.org/10.1016/j.ejmech.2015.11.043.

Language

en

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