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. 2005 Mar 15;13(6):2305-12.
doi: 10.1016/j.bmc.2004.12.042.

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

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

Søren Ebdrup et al. Bioorg Med Chem. .

Abstract

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 IC(50) values of 140, 17 and 350 nM, respectively.

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