Identification of a novel boronic acid as a potent, selective, and orally active hormone sensitive lipase inhibitor.
Basic Information
ID: ALA3813600
Journal: Bioorg Med Chem
Title: Identification of a novel boronic acid as a potent, selective, and orally active hormone sensitive lipase inhibitor.
Authors: Ogiyama T, Yamaguchi M, Kurikawa N, Honzumi S, Yamamoto Y, Sugiyama D, Inoue S.
Abstract: Hormone sensitive lipase (HSL) is an attractive therapeutic target of dyslipidemia. We designed and synthesized several compounds as reversible HSL inhibitors with a focus on hydrophobic interactions, which was thought to be effective upon the HSL inhibitory activity. In these efforts, we identified boronated compound 12 showing a potent HSL inhibitory activity with an IC50 value of 7nM and a high selectivity against cholinesterases. Furthermore, compound 12 is the first boron containing HSL inhibitor that has shown an antilipolytic effect in rats after oral administration at 3mg/kg.
CiteXplore: 27338659
DOI: 10.1016/j.bmc.2016.06.022
Patent ID: ┄