Discovery and synthesis of tetrahydropyrimidinedione-4-carboxamides as endothelial lipase inhibitors.

Bioorganic & Medicinal Chemistry Letters(2018)

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摘要
•A series of tetrahydropyrimidinedione EL inhibitors was identified.•New compounds showed measurable EL inhibition in human serum.•Optimization led to 4a with micromolar human serum potency and 3g with acceptable mouse PK.
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关键词
Endothelial lipase (EL) inhibitors,Tetrahydropyrimidinedione (THP),High density lipoprotein cholesterol (HDL-C),Atherosclerosis
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