Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes.
Bhambra, AS; Edgar, M; Elsegood, MR; Li, Y; Weaver, GW; Arroo, RR; Yardley, V
; Burrell-Saward, H; Krystof, V and
(2015)
Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes.
European journal of medicinal chemistry, 108.
pp. 347-353.
ISSN 0223-5234
DOI: 10.1016/j.ejmech.2015.11.043
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.
Item Type | Article |
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ISI | 369191800029 |
Date Deposited | 04 Jan 2016 20:08 |
ORCID: https://orcid.org/0009-0005-3744-7003