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Induction of cytochrome P-450 by alcohols and 4-substituted pyrazoles

Authors :
Neal W. Cornell
Jacqueline F. Sinclair
Corwin Hansch
Linda Zaitlin
Source :
Biochemical Pharmacology. 35:707-710
Publication Year :
1986
Publisher :
Elsevier BV, 1986.

Abstract

A comparison was made between 4-substituted pyrazoles and short-chain alcohols as inducers of cytochrome P-450. A quantitative structure-activity analysis of the data led to the following equations: (I) Pyrazoles: Log 1/C = 0.85 (±0.21) Log P + 1.93 (±0.38), r = 0.970 (II) Alcohols: Log l /C = 0.78 (±0.14) Log P + 1.46 (±0.13), r = 0.988 where C is the concentration that caused a 50% increase in cytochrome P-450, P is the partition coefficient between octanol and water, and r is the correlation coefficient. The results suggest that induction of cytochrome P-450 by these compounds depends on hydrophobicity alone. Electronic and steric factors have insignificant roles.

Details

ISSN :
00062952
Volume :
35
Database :
OpenAIRE
Journal :
Biochemical Pharmacology
Accession number :
edsair.doi...........b0b27d9745b108ac13e73507f3ff20af
Full Text :
https://doi.org/10.1016/0006-2952(86)90370-9