Synthesis and antiprotozoal activity of novel 2-{[2-(1H-imidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole derivatives |
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Authors: | Jaime Pérez-Villanueva Alicia Hernández-Campos Lilián Yépez-Mulia Carlos Méndez-Cuesta Oscar Méndez-Lucio Francisco Hernández-Luis Rafael Castillo |
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Affiliation: | 1. Facultad de Química, Departamento de Farmacia, UNAM, DF 04510, Mexico;2. Unidad de Investigación Médica en Enfermedades Infecciosas y Parasitarias, IMSS, DF 06720, Mexico |
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Abstract: | A series of 19 new 2-{[2-(1H-imidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole derivatives was synthesized starting from the properly substituted 1,2-phenylendiamine. These compounds have hydrogen or methyl at position 1; while hydrogen, chlorine, ethoxy or methoxycarbonyl group is at position 5 and/or 6. The novel compounds were tested against protozoa Trichomonas vaginalis, Giardia intestinalis and Entamoeba histolytica. Experimental evaluations revealed strong activity for all tested compounds, having IC50 values in the nanomolar range, which were even better than metronidazole, the drug of choice for these parasites. |
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Keywords: | Benzimidazole |
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