Discovery and synthesis of tetrahydropyrimidinedione-4-carboxamides as endothelial lipase inhibitors.
Bioorganic & Medicinal Chemistry Letters(2018)
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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