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Keywords:

  • 2-hydrazolyl-4-thiazolidinone;
  • Chagas disease;
  • cruzipain;
  • inhibitors;
  • multicomponent connection reaction;
  • Trypanosoma cruzi

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.