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.
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Synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma Cruzi.
Chem Biol Drug Des
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Departamento de Química Orgánica, Cátedra de Química Farmacéutica, Universidad de la República (UdelaR), Avda. General Flores 2124, CC1157 Montevideo, Uruguay.
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.
View Article and Find Full Text PDFMicrowave assisted tandem reactions for the synthesis of 2-hydrazolyl-4-thiazolidinones.
Tetrahedron Lett
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Laboratorio de Química Farmacéutica, DQO, Facultad de Química, Universidad de la República, Gral Flores 2124, CC 1157, Montevideo Uruguay.
A tandem method for the synthesis of 2-hydrazolyl-4-thiazolidinones (5) from commercially available materials in a 3 component reaction has been developed. The reaction connects aldehydes, thiosemicarbazides and maleic anhydride, effectively assisted by microwave irradiation. The synthesis of a new type of compound, 2-hydrazolyl-5,5-diphenyl-4-thiazolidinone (7), obtained by treatment of thiosemicarbazone with benzil in basic media is also reported.
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