The pattern of fluorine substitution affects binding affinity in a small library of fluoroaromatic inhibitors for carbonic anhydrase

被引：48

作者：

Doyon, JB ^{[1
]}

Jain, A ^{[1
]}

机构：

[1] Swarthmore Coll, Dept Chem, Swarthmore, PA 19081 USA

来源：

ORGANIC LETTERS | 1999年 / 1卷 / 02期

关键词：

D O I：

10.1021/ol9905250

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A library of fluoroaromatic inhibitors of carbonic anhydrase has been found to bind in a manner dependent on both hydrophobicity and the pattern of substitution of the fluoroaromatic ring. All of the compounds in the library bind to the protein with K-d < 3 nM. We have inferred;two distinct binding modes from our data, which suggest two types of interactions that should be considered when designing fluorinated drugs.

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页码：183 / 185

页数：3

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