Synthesis and antiparasitic activity of 2-(trifluoromethyl)-benzimidazole derivatives.
2-(Trifluoromethyl)benzimidazole derivatives substituted at the 1-, 5-, and 6-positions have been synthesized and in vitro tested against the protozoa Giardia lamblia, Entamnoeha histolytica. and the helminth Trichinella spiralis. Results indicate that all the compounds tested are more active as antiprotozoal agents than Albendazole and Metronidazole. One compound (20) was as active as Albendazole against T. spiralis. These compounds were also tested for their effect on tubulin polymerization and none inhibited tubulin polymerization.
Navarrete-Vázquez
G
G
Departamento de Farmacia, Facultad de Química, UNAM, CU, Mexico D.F.
Cedillo
R
R
Hernández-Campos
A
A
Yépez
L
L
Hernädez-Luis
F
F
Valdez
J
J
Morales
R
R
Cortés
R
R
Hernández
M
M
Castillo
R
R
D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001923:Brain Chemistry / Q000187:drug effects; D004748:Entamoeba histolytica / Q000187:drug effects; D017611:Fluorine Compounds / Q000737:chemistry; D016829:Giardia lamblia / Q000187:drug effects; D007814:Larva / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D017160:Trichinella spiralis / Q000187:drug effects; D014404:Tubulin / Q000187:drug effects
D000977:Antiparasitic Agents; D001562:Benzimidazoles; D017611:Fluorine Compounds; D014404:Tubulin