Synthesis and antiprotozoal activity of novel 1-methylbenzimidazole derivatives.
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.
Valdez-Padilla
David
D
Departamento de Farmacia, Facultad de Química, UNAM, México, DF, Mexico.
Rodríguez-Morales
Sergio
S
Hernández-Campos
Alicia
A
Hernández-Luis
Francisco
F
Yépez-Mulia
Lilián
L
Tapia-Contreras
Amparo
A
Castillo
Rafael
R
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
D000981:Antiprotozoal Agents; D001562:Benzimidazoles