title: Synthesis and antiprotozoal activity of novel 2-{[2-(1H-imidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole derivatives.
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.
authors.affiliation: Facultad de Química, Departamento de Farmacia, UNAM, DF 04510, Mexico.
authors.forename: Jaime
authors.initials: J
authors.lastname: Pérez-Villanueva
authors.forename: Alicia
authors.initials: A
authors.lastname: Hernández-Campos
authors.forename: Lilián
authors.initials: L
authors.lastname: Yépez-Mulia
authors.forename: Carlos
authors.initials: C
authors.lastname: Méndez-Cuesta
authors.forename: Oscar
authors.initials: O
authors.lastname: Méndez-Lucio
authors.forename: Francisco
authors.initials: F
authors.lastname: Hernández-Luis
authors.forename: Rafael
authors.initials: R
authors.lastname: Castillo
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D004748:Entamoeba histolytica / Q000187:drug effects; D016829:Giardia lamblia / Q000187:drug effects; D008795:Metronidazole / Q000494:pharmacology; D010655:Phenylenediamines / Q000737:chemistry; D013329:Structure-Activity Relationship; D014246:Trichomonas vaginalis / Q000187:drug effects
chemical_list: D000981:Antiprotozoal Agents; D001562:Benzimidazoles; D010655:Phenylenediamines; D008795:Metronidazole; C034193:1,2-diaminobenzene; C031000:benzimidazole