Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 86, Issue -, Pages 48-59Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.08.012
Keywords
Chagas disease; Tiypanosoma cruzi; Thiazoles; Hydrazones; 2-Pyridine thiosemicarbazone
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Funding
- Brazilian National Research Council (CNPq)
- Research Foundation of Pernambuco State (FACEPE)
- FIOCRUZ
- FACEPE scholarship
- FAPESB scholarship
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The present work reports on the synthesis, anti-Trypanosoma cruzi activities and docking studies of a novel series of 2-(pyridin-2-yl)-1,3-thiazoles derived from 2-pyridine thiosemicarbazone. The majority of these compounds are potent cruzain inhibitors and showed excellent inhibition on the trypomastigote form of the parasite, and the resulting structure-activity relationships are discussed. Together, these data present a novel series of thiazolyl hydrazones with potential effects against Chagas disease and they could be important leads in continuing development against Chagas disease. (c) 2014 Elsevier Masson SAS. All rights reserved.
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