Synthesis and antiprotozoal activity of some 2-(trifluoromethyl)-1H-benzimidazole bioisosteres

…, M de Monserrat Rojano-Vilchis, L Yépez-Mulia…

文献索引：Navarrete-Vazquez, Gabriel; Rojano-Vilchis, Maria De Monserrat; Yepez-Mulia, Lilian; Melendez, Victor; Gerena, Lucia; Hernandez-Campos, Alicia; Castillo, Rafael; Hernandez-Luis, Francisco European Journal of Medicinal Chemistry, 2006 , vol. 41, # 1 p. 135 - 141

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被引用次数: 78

摘要

A series of 2-(trifluoromethyl)-1H-benzimidazole derivatives with various 5-and 6-position bioisosteric substituents (–Cl,–F,–CF3,–CN), namely 1–7, were prepared using a short synthetic route. Each analogue was tested in vitro against the protozoa Giardia intestinalis and Trichomonas vaginalis in comparison with albendazole and metronidazole. Several analogues had IC50 values< 1 μM against both species, which make them significantly ...