Synthesis of 2-Hydrazolyl-4-Thiazolidinones Based on Multicomponent Reactions and Biological Evaluation Against Trypanosoma Cruzi

Autor: Cecilia Saiz, Graciela Mahler, Agustina Chidichimo, Luis Enrique Bruno Blanch, Alan Talevi, Diego Benítez, Peter Wipf, Pablo Hernán Palestro, Carolina Leticia Bellera, Luciana Gavernet, Chiara Pizzo, Juan José Cazzulo
Rok vydání: 2011
Předmět:
Zdroj: Chemical Biology & Drug Design. 77:166-172
ISSN: 1747-0277
DOI: 10.1111/j.1747-0285.2010.01071.x
Popis: 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 μm 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.
Databáze: OpenAIRE