Synthesis and antiparasitic activity of 1H-benzimidazole derivatives.
Compounds 1-18 have been synthesized and tested in vitro against the protozoa Giardia lamblia, Entamoeba histolytica and the helminth Trichinella spiralis. Inhibition of rat brain tubulin polymerization was also measured and compared for each compound. Results indicate that most of the compounds tested were more active as antiprotozoal agents than Metronidazole and Albendazole. None of the compounds was as active as Albendazole against T. spiralis. Although only compounds 3, 9 and 15 (2-methoxycarbonylamino derivatives) inhibited tubulin polymerization, these were not the most potent antiparasitic compounds.
Departamento de Farmacia, Facultad de Química, UNAM, CU. 04510, México D.F., Mexico.
Juan
J
Valdez
Roberto
R
Cedillo
Alicia
A
Hernández-Campos
Lilián
L
Yépez
Francisco
F
Hernández-Luis
Gabriel
G
Navarrete-Vázquez
Amparo
A
Tapia
Rafael
R
Cortés
Manuel
M
Hernández
Rafael
R
Castillo
D015766:Albendazole / Q000494:pharmacology; D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001921:Brain; D056890:Eukaryota / Q000187:drug effects; D008795:Metronidazole / Q000494:pharmacology; D015394:Molecular Structure; D051381:Rats; D017160:Trichinella spiralis / Q000187:drug effects; D014404:Tubulin / Q000378:metabolism
D000977:Antiparasitic Agents; D001562:Benzimidazoles; D014404:Tubulin; D008795:Metronidazole; D015766:Albendazole