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Synthesis and antiparasitic activity of albendazole and mebendazole analogues
Authors:Navarrete-Vázquez Gabriel  Yépez Lilián  Hernández-Campos Alicia  Tapia Amparo  Hernández-Luis Francisco  Cedillo Roberto  González José  Martínez-Fernández Antonio  Martínez-Grueiro Mercedes  Castillo Rafael
Affiliation:Departamento de Farmacia, Facultad de Química, UNAM, CU, DF 04510, Mexico. gabriel_navarrete@correo.unam.mx
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.
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