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|Title: ||Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-Trifluorobenzothiophenes|
|Authors: ||Bhambra, Avninder S.|
Elsegood, Mark R.J.
Weaver, George W.
Arroo, Randolph R.J.
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|
|Publisher Link: ||http://dx.doi.org/10.1016/j.ejmech.2015.11.043|
|Appears in Collections:||Published Articles (Chemistry)|
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