Structure-activity correlations in the metabolism of drugs

doi:10.1016/0003-9861(68)90038-6

Archives of Biochemistry and Biophysics

Volume 128, Issue 2, November 1968, Pages 319-330

https://doi.org/10.1016/0003-9861(68)90038-6 Get rights and content

Abstract

Substituent constants and regression analysis have been employed in the study of metabolism of organic compounds. Most of the variation in the structure-activity relationship appears to be associated with relative lipophilic character of the derivatives as defined by octanol-water partition coefficients. The ideal lipophilic character for amines undergoing metabolism by crude monoamine oxidase is defined by log P₀ = 2. This same constant also applies to the formation of glucuronides by alcohols and benzoic acids and hippuric acid formation by benzoic acids.

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^☆: This work was supported by Research Grant GM-07492 from the National Institutes of Health.

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Structure-activity correlations in the metabolism of drugs☆

Abstract

Biochem. Pharmacol

Biochem. Pharcol

J. Biol. Chem

Farmaco

J. Am. Chem. Soc

Biochemistry

Angew. Chem

J. Am. Chem. Soc

Mol. Pharmacol

J. Med. Chem

J. Med. Chem

The Permeability of Natural Membranes

Biochim. Biophys. Acta

Rates and Equilibria of Organic Reactions