Synthesis and antiparasitic activity of albendazole and mebendazole analogues.

Author(s): Navarrete-Vazquez G, Yepez L, Hernandez-Campos A, Tapia A, Hernandez-Luis F, Cedillo R, Gonzalez J, Martinez-Fernandez A, Martinez-Grueiro M, Castillo R

Affiliation(s): Departamento de Farmacia, Facultad de Quimica, UNAM, CU, DF 04510, Mexico. gabriel_navarrete@correo.unam.mx

Publication date & source: 2003-10-15, Bioorg Med Chem., 11(21):4615-22.

Publication type:

Albendazole (Abz) and Mebendazole (Mbz) analogues have been synthesized and in vitro tested against the protozoa Giardia lamblia, Trichomonas vaginalis and the helminths Trichinella spiralis and Caenorhabditis elegans. Results indicate that compounds 4a, 4b (Abz analogues), 12b and 20 (Mbz analogues) are as active as antiprotozoal agents as Metronidazole against G. lamblia. Compound 9 was 58 times more active than Abz against T. vaginalis. Compounds 8 and 4a also shown high activity against this protozoan. Compounds 4b and 5a were as active as Abz. None of the Mbz analogues showed activity against T. vaginalis. The anthelmintic activity presented by these compounds was poor.