AB 23-11-15 Manuscript[2].pdf (356.55 kB)
Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-Trifluorobenzothiophenes
journal contribution
posted on 2015-12-11, 14:09 authored by Avninder S. Bhambra, Mark Edgar, Mark ElsegoodMark Elsegood, Yuqi Li, George WeaverGeorge Weaver, Randolph R.J. Arroo, Vanessa Yardley, Hollie Burrell-Saward, Vladimir KrystofCurrent 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 ChemistryCitation
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
© ElsevierVersion
- 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
2016Notes
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.Publisher version
Language
- en