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Novel antiprotozoal products: imidazole and benzimidazole N-oxide derivatives and related compounds |
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| Authors: | Aguirre Gabriela Boiani Mariana Cerecetto Hugo Gerpe Alejandra González Mercedes Sainz Yolanda Fernández Denicola Ana De Ocáriz Carmen Ochoa Nogal Juan José Montero David Escario José Antonio |
| Affiliation: | Departamento de Química Orgánica, Facultad de Química-Facultad de Ciencias, Montevideo, Uruguay. |
| Abstract: | The syntheses and biological evaluation of the first anti-protozoa imidazole N-oxide and benzimidazole N-oxide and their derivatives are reported. They were tested in vitro against two different protozoa, Trypanosoma cruzi and Trichomonas vaginalis. Derivative 7c, ethyl-1-(i-butyloxycarbonyloxy)-6-nitrobenzimid-azole-2-carboxylate, displayed activity on both protozoa. Lipophilicity and redox potential were experimentally determined in order to study the relationship with activity of the compounds. These properties are well related with the observed bioactivity. Imidazole and benzimidazole N-oxide derivatives are becoming leaders for further chemical modifications and advanced biological studies. |
| Keywords: | Anti‐protozoa compounds Imidazole N‐oxide Structure‐activity relationship |
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