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Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes
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SYSNO ASEP 0459007 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes Author(s) Bhambra, A.S. (GB)
Edgar, M. (GB)
Elsegood, M.R.J. (GB)
Li, Y. (GB)
Weaver, G.W. (GB)
Arroo, R.R.J. (GB)
Yardley, V. (JP)
Burrell-Saward, H. (GB)
Kryštof, Vladimír (UEB-Q) RID, ORCIDSource Title European Journal of Medicinal Chemistry. - : Elsevier - ISSN 0223-5234
Roč. 108, JAN 27 (2016), s. 347-353Number of pages 7 s. Language eng - English Country FR - France Keywords Benzothiophenes ; Fluorinated drugs ; Antitrypanosomal activity Subject RIV EB - Genetics ; Molecular Biology R&D Projects LO1204 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Institutional support UEB-Q - RVO:61389030 UT WOS 000369191800029 DOI 10.1016/j.ejmech.2015.11.043 Annotation 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 mu M) against Trypanosoma brucei rhodesiense and no toxicity towards mammalian cells. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2017
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