Design,synthesis, and in vitro antiprotozoal,antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas |
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| Authors: | Carlos Nava-Zuazo Samuel Estrada-Soto Jorge Guerrero-Álvarez Ismael León-Rivera Gloria María Molina-Salinas Salvador Said-Fernández Manuel Jesús Chan-Bacab Roberto Cedillo-Rivera Rosa Moo-Puc Gumersindo Mirón-López Gabriel Navarrete-Vazquez |
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| Institution: | 1. Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico;2. Centro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico;3. División de Biología Celular y Molecular, Centro de Investigación Biomédica del Noreste, IMSS, Monterrey, Nuevo León 64720, Mexico;4. Departamento de Microbiología Ambiental y Biotecnología, Universidad Autónoma de Campeche, Campeche 24030, Mexico;5. Unidad de Investigación Médica Yucatán, Unidad Médica de Alta Especialidad del Centro Médico Nacional Ignacio García Téllez, IMSS Mérida, Yucatán 97000, Mexico;6. Facultad de Química, Universidad Autónoma de Yucatán, Merida, Yucatán 97000, Mexico |
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| Abstract: | We have synthesized a new series of quinoline tripartite hybrids from chloroquine, ethambutol, and isoxyl drugs, using a short synthetic route. Compounds 1–8 were tested in vitro against five protozoa (Giardia intestinalis, Trichomonas vaginalis, Entamoeba histolytica, Leishmania mexicana and Trypanosoma cruzi) and Mycobacterium tuberculosis. N-(4-Butoxyphenyl)-N′-{2-(7-chloroquinolin-4-yl)amino]ethyl}urea (6) was the most active compound against all parasites tested. Compound 6 was 670 times more active than metronidazole, against G. intestinalis. It was as active as pentamidine against L. mexicana, and it was twofold more potent than ethambutol and isoxyl versus M. tuberculosis. This compound could be considered as a new broad spectrum antimicrobial agent. |
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