Estrada-Soto Samuel, Villalobos-Molina Rafael, Aguirre-Crespo Francisco, Vergara-Galicia Jorge, Moreno-Díaz Hermenegilda, Torres-Piedra Mariana, Navarrete-Vázquez Gabriel
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Mor. 62210, México.
Life Sci. 2006 Jun 27;79(5):430-5. doi: 10.1016/j.lfs.2006.01.019. Epub 2006 Feb 17.
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 microM (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.
利用体外大鼠主动脉环试验记录了具有各种5-和6-位取代基（-H、-CH3、-NO2、-CF3）的2-（邻、对取代苯基）-1H-苯并咪唑衍生物（即1-7）的舒张活性。化合物3和6 [2-（5-硝基-1H-苯并咪唑-2-基）苯酚和2-（4-甲氧基苯基）-5-硝基-1H-苯并咪唑]采用短路线制备，是该系列中最有效的化合物，其IC50值分别为0.95和1.41（有内皮）以及2.01和3.61微摩尔（无内皮）。通过在这些苯并咪唑衍生物中使用生物电子等排体取代来进一步研究构效关系，应能提供新型血管舒张先导物，并可能用于对抗高血压疾病。
