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

Authors

  • Chiara Pizzo,

    1. Departamento de Química Orgánica, Cátedra de Química Farmacéutica, Universidad de la República (UdelaR), Avda. General Flores 2124, CC1157 Montevideo, Uruguay
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  • Cecilia Saiz,

    1. Departamento de Química Orgánica, Cátedra de Química Farmacéutica, Universidad de la República (UdelaR), Avda. General Flores 2124, CC1157 Montevideo, Uruguay
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  • Alan Talevi,

    1. Cátedra de Química Medicinal, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata (UNLP), La Plata, Argentina
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  • Luciana Gavernet,

    1. Cátedra de Química Medicinal, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata (UNLP), La Plata, Argentina
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  • Pablo Palestro,

    1. Cátedra de Química Medicinal, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata (UNLP), La Plata, Argentina
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  • Carolina Bellera,

    1. Cátedra de Química Medicinal, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata (UNLP), La Plata, Argentina
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  • Luis Bruno Blanch,

    1. Cátedra de Química Medicinal, Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata (UNLP), La Plata, Argentina
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  • Diego Benítez,

    1. Laboratorio de Química Orgánica, Facultad de Ciencias-Facultad de Química, UdelaR, Montevideo, Uruguay
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  • Juan J. Cazzulo,

    1. IIB-INTECH Universidad Nacional de General San Martín – CONICET, San Martín, Argentina
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  • Agustina Chidichimo,

    1. IIB-INTECH Universidad Nacional de General San Martín – CONICET, San Martín, Argentina
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  • Peter Wipf,

    1. Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA
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  • S. Graciela Mahler

    Corresponding author
    1. Departamento de Química Orgánica, Cátedra de Química Farmacéutica, Universidad de la República (UdelaR), Avda. General Flores 2124, CC1157 Montevideo, Uruguay
      Corresponding author: S. Graciela Mahler,gmahler@fq.edu.uy
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Corresponding author: S. Graciela Mahler,gmahler@fq.edu.uy

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.

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