posted on 2015-12-11, 14:09authored byAvninder S. Bhambra, Mark 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.
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.
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.