Synthesis and antiparasitic activity of albendazole and mebendazole analogues.
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.
Navarrete-Vázquez
Gabriel
G
Departamento de Farmacia, Facultad de Química, UNAM, CU, DF 04510, Mexico. gabriel_navarrete@correo.unam.mx
Yépez
Lilián
L
Hernández-Campos
Alicia
A
Tapia
Amparo
A
Hernández-Luis
Francisco
F
Cedillo
Roberto
R
González
José
J
Martínez-Fernández
Antonio
A
Martínez-Grueiro
Mercedes
M
Castillo
Rafael
R
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
D000977:Antiparasitic Agents; D008795:Metronidazole; D008463:Mebendazole; D015766:Albendazole