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Bioorganic & medicinal chemistry

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


PMID 24211162

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.

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455253
2-Fluoro-5-(trifluoromethyl)benzoic acid, 98%
C8H4F4O2
SML1324 XEN445, ≥98% (HPLC)
C18H17F3N2O3