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Synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma Cruzi |
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| Authors: | 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 |
| Affiliation: | Departamento de Química Orgánica, Cátedra de Química Farmacéutica, Universidad de la República (UdelaR), Avda. General Flores 2124, CC1157 Montevideo, Uruguay. |
| Abstract: | 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. |
| Keywords: | 2‐hydrazolyl‐4‐thiazolidinone Chagas disease cruzipain inhibitors multicomponent connection reaction Trypanosoma cruzi |
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