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Bioorg Med Chem. 2013 Dec 15;21(24):7724-34. doi: 10.1016/j.bmc.2013.10.023. Epub 2013 Oct 28.

Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice.

Author information

1
Xenon Pharmaceuticals Inc, 200-3650 Gilmore Way, Burnaby, BC V5G 4W8, Canada. Electronic address: ssun@xenon-pharma.com.

Abstract

Endothelial lipase (EL) activity has been implicated in HDL metabolism and in atherosclerotic plaque development; inhibitors are proposed to be efficacious in the treatment of dyslipidemia related cardiovascular disease. We describe here the discovery of a novel class of anthranilic acids EL inhibitors. XEN445 (compound 13) was identified as a potent and selective EL inhibitor, that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.

KEYWORDS:

Anthranilic acid; Cardiovascular disease; Endothelial lipase inhibitors; HDL cholesterol

PMID:
24211162
DOI:
10.1016/j.bmc.2013.10.023
[Indexed for MEDLINE]

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