title: Synthesis and antiparasitic activity of albendazole and mebendazole analogues.
abstract: 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.
authors.affiliation: Departamento de Farmacia, Facultad de Química, UNAM, CU, DF 04510, Mexico. gabriel_navarrete@correo.unam.mx
authors.forename: Gabriel
authors.initials: G
authors.lastname: Navarrete-Vázquez
authors.forename: Lilián
authors.initials: L
authors.lastname: Yépez
authors.forename: Alicia
authors.initials: A
authors.lastname: Hernández-Campos
authors.forename: Amparo
authors.initials: A
authors.lastname: Tapia
authors.forename: Francisco
authors.initials: F
authors.lastname: Hernández-Luis
authors.forename: Roberto
authors.initials: R
authors.lastname: Cedillo
authors.forename: José
authors.initials: J
authors.lastname: González
authors.forename: Antonio
authors.initials: A
authors.lastname: Martínez-Fernández
authors.forename: Mercedes
authors.initials: M
authors.lastname: Martínez-Grueiro
authors.forename: Rafael
authors.initials: R
authors.lastname: Castillo
mesh_terms: D015766:Albendazole / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D017173:Caenorhabditis elegans / Q000187:drug effects; D016829:Giardia lamblia / Q000187:drug effects; D008463:Mebendazole / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D008795:Metronidazole / Q000627:therapeutic use
chemical_list: D000977:Antiparasitic Agents; D008795:Metronidazole; D008463:Mebendazole; D015766:Albendazole