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Synthesis of 2‐Hydrazolyl‐4‐Thiazolidinones Based on Multicomponent Reactions and Biological Evaluation Against Trypanosoma Cruzi
Author(s) -
Pizzo Chiara,
Saiz Cecilia,
Talevi Alan,
Gavernet Luciana,
Palestro Pablo,
Bellera Carolina,
Blanch Luis Bruno,
Benítez Diego,
Cazzulo Juan J.,
Chidichimo Agustina,
Wipf Peter,
Mahler S. Graciela
Publication year - 2011
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2010.01071.x
Subject(s) - trypanosoma cruzi , chemistry , biological activity , in vitro , combinatorial chemistry , biochemistry , parasite hosting , world wide web , computer science
A series of 18 novel 2‐hydrazolyl‐4‐thiazolidinones‐5‐carboxylic acids, amides and 5,6‐α,β‐unsaturated esters were synthesized, and their in vitro activity on cruzipain and T. cruzi epimastigotes was determined. Some agents show activity at 37 μ m concentration in the enzyme assay. Computational tools and docking were used to correlate the biological response with the physicochemical parameters of the compounds and their cruzipain inhibitory effects.