title: Synthesis and antiprotozoal activity of novel 1-methylbenzimidazole derivatives.
abstract: In this paper are reported the synthesis and antiprotozoal activity in vitro of 24 1-methylbenzimidazole derivatives (13-36) substituted at position 2 with aminocarbonyl, N-methylaminocarbonyl, N,N-dimethylaminocarbonyl, ethoxycarbonyl, 1-hydroxyethyl and acetyl groups, some of them with chlorine atoms at the benzenoid ring. Compounds 13-36 were more active than metronidazole, the choice drug against Giardia intestinalis and most of them against Trichomonas vaginalis. The most active group of compounds for both parasites was that with a 2-ethoxycarbonyl group (16, 22, 28, 34), independently of the substitution pattern at the benzenoid ring.
authors.affiliation: Departamento de Farmacia, Facultad de Química, UNAM, México, DF, Mexico.
authors.forename: David
authors.initials: D
authors.lastname: Valdez-Padilla
authors.forename: Sergio
authors.initials: S
authors.lastname: Rodríguez-Morales
authors.forename: Alicia
authors.initials: A
authors.lastname: Hernández-Campos
authors.forename: Francisco
authors.initials: F
authors.lastname: Hernández-Luis
authors.forename: Lilián
authors.initials: L
authors.lastname: Yépez-Mulia
authors.forename: Amparo
authors.initials: A
authors.lastname: Tapia-Contreras
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*; D008826:Microbial Sensitivity Tests; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D001562:Benzimidazoles