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Title: Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-Trifluorobenzothiophenes
Authors: Bhambra, Avninder S.
Edgar, Mark
Elsegood, Mark R.J.
Li, Yuqi
Weaver, George W.
Arroo, Randolph R.J.
Yardley, Vanessa
Burrell-Saward, Hollie
Krystof, Vladimir
Keywords: Benzothiophenes
Fluorinated drugs
Antitrypanosomal activity
Sleeping sickness
Human African Trypanosomiasis
Trypanosoma brucei rhodesiense
Issue Date: 2016
Publisher: © Elsevier
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.
Abstract: 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.
Description: 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.
Sponsor: 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.
Version: Accepted for publication
DOI: 10.1016/j.ejmech.2015.11.043
URI: https://dspace.lboro.ac.uk/2134/19829
Publisher Link: http://dx.doi.org/10.1016/j.ejmech.2015.11.043
Appears in Collections:Published Articles (Chemistry)

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