Structure-activity relationship for aryl and heteroaryl boronic acid inhibitors of hormone-sensitive lipase
Structure-activity relationship for aryl and heteroaryl boronic acid inhibitors of hormone-sensitive lipase
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DOI：
10.1016/j.bmc.2004.12.042
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发表时间：
2005-03-15
影响因子：
3.5
通讯作者：
Vedso, P
中科院分区：
文献类型：
--
作者：
Ebdrup, S;Jacobsen, P;Vedso, P
测试了一系列芳基和杂芳基硼酸的体外激素敏感性脂肪酶抑制特性。 (2-苄氧基-5-氟苯基)硼酸、(2-苄氧基-5-氯苯基)硼酸和5-溴噻吩-2-硼酸被发现是最有效的HSL抑制剂，IC50值分别为140、17和350 nm。 (c) 2004 Elsevier Ltd. 保留所有权利。
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.