Structure-activity relationship for aryl and heteroaryl boronic acid inhibitors of hormone-sensitive lipase

被引：35

作者：

Ebdrup, S ^{[1
]}

Jacobsen, P ^{[1
]}

Farrington, AD ^{[1
]}

Vedso, P ^{[1
]}

机构：

[1] Novo Nordisk AS, DK-2760 Malov, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 06期

关键词：

D O I：

10.1016/j.bmc.2004.12.042

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A range of aryl and heteroaryl boronic acids were tested for their in vitro hormone-sensitive lipase inhibitory properties. (2-Benzyloxy-5-fluorophenyl)boronic acid, (2-benzyloxy-5-chlorophenyl)boronic acid and 5-bromothiophene-2-boronic acid were found to be the most potent HSL inhibitors with IC50 values of 140, 17 and 350 nm, respectively. (c) 2004 Elsevier Ltd. All rights reserved.

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页码：2305 / 2312

页数：8

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