Structure-Metabolism Relationships Steric Effects and the Enzymatic Hydrolysis of Carboxylic Esters

Author: Buchwald P.

Source: Mini Reviews in Medicinal Chemistry, Volume 1, Number 1, May 2001 , pp. 101-111(11)

Publisher: Bentham Science Publishers

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Abstract:

After a brief review of a number of issues related to the enzymatic hydrolysis of carboxylic esters, such as interspecies variability, mechanism, stereospecificity, and activation energy, and after an overview of relevant aspects related to the quantitative modeling of steric effects, the results of a recently developed quantitative structure-metabolism relationship model are discussed. They were obtained for in vitro human blood enzymatic hydrolysis of noncongener esters by introduction of the inaccessible solid angle as a novel measure of steric hindrance.

Keywords: Structure Metabolism Relationships; Steric Effects; Enzymatic Hydrolysis; noncongener esters; quantitative structure-metabolism relationships; esterase activity; enantioselectivity; liposomal phosphatidylcholine; pharmacokinetic studies; Multiple halosubstituted

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557013407403

Publication date: 2001-05-01

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The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines.

The scope of Mini-Reviews in Medicinal Chemistry will cover all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies.

Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.