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Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas

2010; Elsevier BV; Volume: 18; Issue: 17 Linguagem: Inglês

10.1016/j.bmc.2010.07.008

1464-3391

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‐Vázquez,

Research on Leishmaniasis Studies

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.