Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES)

被引：28

作者：

Ahmed, S ^{[1
]}

Owen, CP ^{[1
]}

James, K ^{[1
]}

Patel, CK ^{[1
]}

Patel, M ^{[1
]}

机构：

[1] Kingston Univ, Sch Chem & Pharmaceut Sci, Kingston upon Thames KT1 2EE, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(01)00087-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the initial results of the synthesis and biochemical evaluation of a series of aminosulfonate based compounds of phenol and the determination of the pK(a) of the parent phenol in an attempt to investigate the role of this physicochemical factor in the irreversible inhibition of the enzyme estrone sulfatase (ES). The results of the study show that there is a strong correlation between the observed pK(a) and inhibitory activity. We postulate that the stability of the phenoxide ion, as indicated by the acid dissociation constant, is an important factor in the irreversible inhibition of this enzyme. (C) 2001 Published by Elsevier Science Ltd.

引用

页码：899 / 902

页数：4

共 8 条

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