Journal of Medicinal Chemistry p. 887 - 892 (1982)
Update date:2022-08-03
Topics:
Murray, Michael
Ryan, Adrian J.
Little, Peter J.
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 structure-activity relationship (QSAR) that describes up to 87percent of the data variance in terms of hydrophobic and electronic effects and the molar refractivity of the substituent in the 2-position of the benzimidazole ring.
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