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2-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation.

Authors :
Cardoso MV
de Siqueira LR
da Silva EB
Costa LB
Hernandes MZ
Rabello MM
Ferreira RS
da Cruz LF
Moreira DR
Pereira VR
de Castro MC
Bernhardt PV
Leite AC
Source :
European journal of medicinal chemistry [Eur J Med Chem] 2014 Oct 30; Vol. 86, pp. 48-59. Date of Electronic Publication: 2014 Aug 06.
Publication Year :
2014

Abstract

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.<br /> (Copyright © 2014 Elsevier Masson SAS. All rights reserved.)

Details

Language :
English
ISSN :
1768-3254
Volume :
86
Database :
MEDLINE
Journal :
European journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
25147146
Full Text :
https://doi.org/10.1016/j.ejmech.2014.08.012