Synthesis,trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones,designed as cruzain inhibitors candidates |
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| Authors: | Nelilma C Romeiro Gabriela Aguirre Paola Hernández Mercedes González Hugo Cerecetto Ignacio Aldana Silvia Pérez-Silanes Antonio Monge Eliezer J Barreiro Lídia M Lima |
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| Institution: | 1. Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio), Faculdade de Farmácia, Universidade Federal do Rio de Janeiro (UFRJ), Rio de Janeiro, PO Box 68024, RJ 21944-970, Brazil;2. Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay;3. Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain |
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| Abstract: | In this paper, we report the structural design, synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazone (NAH) derivatives, planned as cruzain inhibitors candidates, a cysteine protease essential for the survival of Trypanosoma cruzi within the host cell. The salicylaldehyde N-acylhydrazones 7a and 8a presented IC50 values of the same magnitude order than the standard drug nifurtimox (Nfx), when tested in vitro against epimastigote forms of Trypanosoma cruzi (Tulahuen 2 strain) and were non-toxic at the highest assayed doses rendering selectivity indexes (IC50 (macrophages)/IC50 (Trypanosoma cruzi)) of >25 for 7a and >20 for 8a, with IC50 values in macrophages >400 μM. |
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