Quantiative Structure-Activity Relationship Between p-Aminobenzoates and Formation Rate of Cytochrome P450 Metabolic Intermediate Complex

Chem. J. Chinese Universities ›› 1994, Vol. 15 ›› Issue (12): 1807.

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Quantiative Structure-Activity Relationship Between p-Aminobenzoates and Formation Rate of Cytochrome P₄₅₀ Metabolic Intermediate Complex

FU Xu-Chun, LIU Zhi-Qiang, JIANG Hui-Di

Department of Pharmacy, Zhejiang Medical University, Hangzhou, 310006

Received:1993-12-24 Revised:1994-04-21 Online:1994-12-24 Published:1994-12-24

Abstract

Abstract: The formation rates (v) of cytochrome P450 metabolic intermediate complexes for twelve p-aminobenzoates with untreated or phenobarbital pretreated rat hepatic microsomes were tested. both Hansch's method and molecular connectivity method were used to establish their quantitative structure-activity relationship equations. The significant parabolic correlations between the logarithm values of the formation rates (lgv) and the logarithm values of octanol/water partition coefficients of the p-aminobenzoates (lgP) or their first-order valence molecular connectivity indexes (¹χ^ν) were observed.

Key words: Cytochrome P₄₅₀, p-Aminobenzoates, Metabolic intermediate complex, Quantitative structure-activity relationship, Molecular connectivity

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FU Xu-Chun, LIU Zhi-Qiang, JIANG Hui-Di . Quantiative Structure-Activity Relationship Between p-Aminobenzoates and Formation Rate of Cytochrome P₄₅₀ Metabolic Intermediate Complex[J]. Chem. J. Chinese Universities, 1994, 15(12): 1807.

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Quantiative Structure-Activity Relationship Between p-Aminobenzoates and Formation Rate of Cytochrome P₄₅₀ Metabolic Intermediate Complex

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