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Bioorg Med Chem Lett. 2002 Aug 19;12(16):2221-4.

Synthesis and antiparasitic activity of 1H-benzimidazole derivatives.

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Departamento de Farmacia, Facultad de Química, UNAM, CU. 04510, México D.F., Mexico.


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.

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