Potent inhibitors of lipoprotein-associated phospholipase A 2: benzaldehyde O-heterocycle-4-carbonyloxime

…, YD Park, HY Park, IY Jeong, TS Jeong, WS Lee

文献索引：Jeong, Hyung Jae; Park, Yong-Dae; Park, Ho-Yong; Jeong, Il Yun; Jeong, Tae-Sook; Lee, Woo Song Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 21 p. 5576 - 5579

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被引用次数: 20

摘要

A series of multi-substituted oximes were prepared and their potencies for inhibiting lipoprotein-associated phospholipase A2 (Lp-PLA2) activity were evaluated in vitro. Among them, compounds 3a, 3b, and 3m were identified to display a micromolar potency for inhibiting Lp-PLA2 in whole human plasma and isolated human LDL. Based on these results, structure–activity relationship was studied on modification of three parts of R1, R2, ...