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

Sun, Shaoyi; Dean, Richard; Jia, Qi; Zenova, Alla; Zhong, Jing; Grayson, Celene; Xie, Clark; Lindgren, Andrea; Samra, Pritpaul; Sojo, Luis; van Heek, Margaret; Lin, Linus; Percival, David; Fu, Jian-Min; Winther, Michael D; Zhang, Zaihui

Sun, Shaoyi; Dean, Richard; Jia, Qi; Zenova, Alla; Zhong, Jing; Grayson, Celene; Xie, Clark; Lindgren, Andrea; Samra, Pritpaul; Sojo, Luis; van Heek, Margaret; Lin, Linus; Percival, David; Fu, Jian-Min; Winther, Michael D; Zhang, Zaihui.

Affiliation

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

Bioorg Med Chem ; 21(24): 7724-34, 2013 Dec 15.

Article in En | MEDLINE | ID: mdl-24211162

Subject(s)

Benzoates/pharmacology; Cholesterol, HDL/blood; Cholesterol, HDL/drug effects; Drug Discovery; Enzyme Inhibitors/pharmacology; Lipase/antagonists & inhibitors; Pyrrolidines/pharmacology; Animals; Benzoates/chemical synthesis; Benzoates/chemistry; Dose-Response Relationship, Drug; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Lipase/deficiency; Lipase/metabolism; Male; Mice; Mice, Inbred C57BL; Mice, Knockout; Molecular Structure; Pyrrolidines/chemical synthesis; Pyrrolidines/chemistry; Structure-Activity Relationship

Key words

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

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Full text: 1 Database: MEDLINE Main subject: Pyrrolidines / Benzoates / Enzyme Inhibitors / Drug Discovery / Lipase / Cholesterol, HDL Limits: Animals Language: En Year: 2013 Type: Article

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