Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2553945 | Life Sciences | 2006 | 6 Pages |
Abstract
The relaxant activity of 2-(o, p-substituted phenyl)-1H-benzimidazole derivatives with various 5- and 6-position substituents (-H, -CH3, -NO2, -CF3), namely 1-7, was recorded using the in vitro rat aorta ring test. Compounds 3 and 6 [2-(5-nitro-1H-benzimidazol-2-yl)phenol and 2-(4-methoxyphenyl)-5-nitro-1H-benzimidazole] were prepared using a short route, and were the most potent compounds of the series, showing IC50 value of 0.95 and 1.41 (with endothelium) and 2.01 and 3.61 μM (without endothelium), respectively. Studying further structure-activity relationships through the use of bioisosteric substitution in these benzimidazole derivatives should provide novel vasorelaxant leads and possibly against hypertensive diseases.
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Authors
Samuel Estrada-Soto, Rafael Villalobos-Molina, Francisco Aguirre-Crespo, Jorge Vergara-Galicia, Hermenegilda Moreno-DÃaz, Mariana Torres-Piedra, Gabriel Navarrete-Vázquez,