Journal of medicinal chemistry

Inhibition of rat hepatic microsomal aminopyrine N-demethylase activity by benzimidazole derivatives. Quantitative structure-activity relationships

M Murray, AJ Ryan, PJ Little

文献索引：Murray, Michael; Ryan, Adrian J.; Little, Peter J. Journal of Medicinal Chemistry, 1982 , vol. 25, # 8 p. 887 - 892

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被引用次数: 55

摘要

Eighty-two benzimidazole derivatives have been prepared and tested for the ability to inhibit cytochrome P-450 mediated enzyme activity (aminopyrine N-demethylase) from phenobarbitone-induced rat hepatic microsomes. Using physicochemical parameters and multiple regression analysis, we derived a quantitative structureactivity relationship (QSAR) that describes up to 87% of the data variance in terms of hydrophobic and electronic ...