Design, Synthesis and Antitrypanosomal Activities of 2,6-Disubstituted-4,5,7-Trifluorobenzothiophenes

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dc.contributor.authorBhambra, Avninder S.en
dc.contributor.authorEdgar, Marken
dc.contributor.authorElsegood, Mark R. J.en
dc.contributor.authorLi, Yuqien
dc.contributor.authorWeaver, George W.en
dc.contributor.authorArroo, R. R. J.en
dc.contributor.authorYardley, Vanessaen
dc.contributor.authorBurrell-Saward, Hollieen
dc.contributor.authorKrystof, Vladimiren
dc.date.accessioned2015-12-14T11:31:28Z
dc.date.available2015-12-14T11:31:28Z
dc.date.issued2015-11-30
dc.description.abstractCurrent 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.en
dc.funderLoughborough Universityen
dc.funderDe Montfort Universityen
dc.identifier.citationBhambra, A.S., Edgar, M., Elsegood, M.R.J. et al. (2016) Design, Synthesis and Antitrypanosomal Activities of 2,6-Disubstituted-4,5,7-Trifluorobenzothiophenes. European Journal of Medicinal Chemistry, online firsten
dc.identifier.doihttps://doi.org/10.1016/j.ejmech.2015.11.043
dc.identifier.urihttp://hdl.handle.net/2086/11403
dc.language.isoenen
dc.peerreviewedYesen
dc.projectidInternalen
dc.publisherElsevieren
dc.researchinstituteInstitute for Allied Health Sciences Researchen
dc.researchinstituteLeicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)en
dc.subjectBenzothiophenesen
dc.subjectFluorinated drugsen
dc.subjectAntitrypanosomal activityen
dc.subjectSleeping sicknessen
dc.subjectHuman African trypanosomiasisen
dc.titleDesign, Synthesis and Antitrypanosomal Activities of 2,6-Disubstituted-4,5,7-Trifluorobenzothiophenesen
dc.typeArticleen

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