%0 Journal Article %A Bhambra, Avninder S. %A Edgar, Mark %A Elsegood, Mark %A Li, Yuqi %A Weaver, George %A Arroo, Randolph R.J. %A Yardley, Vanessa %A Burrell-Saward, Hollie %A Krystof, Vladimir %D 2015 %T Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-Trifluorobenzothiophenes %U https://repository.lboro.ac.uk/articles/journal_contribution/Design_synthesis_and_antitrypanosomal_activities_of_2_6-disubstituted-4_5_7-Trifluorobenzothiophenes/9391139 %2 https://repository.lboro.ac.uk/ndownloader/files/17004656 %K Benzothiophenes %K Fluorinated drugs %K Antitrypanosomal activity %K Sleeping sickness %K Human African Trypanosomiasis %K Trypanosoma brucei rhodesiense %K Chemical Sciences not elsewhere classified %K Organic Chemistry %X 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. %I Loughborough University