N-1取代嘧啶-4-酮：新型口服活性脂蛋白相关磷脂酶A2抑制剂。
N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A2.
作者信息
Boyd H F, Fell S C, Flynn S T, Hickey D M, Ife R J, Leach C A, Macphee C H, Milliner K J, Moores K E, Pinto I L, Porter R A, Rawlings D A, Smith S A, Stansfield I G, Tew D G, Theobald C J, Whittaker C M
机构信息
SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
出版信息
Bioorg Med Chem Lett. 2000 Nov 20;10(22):2557-61. doi: 10.1016/s0960-894x(00)00510-2.
From two related series of 2-(alkylthio)-pyrimidones, a novel series of 1-((amidolinked)-alkyl)-pyrimidones has been designed as nanomolar inhibitors of human lipoprotein-associated phospholipase A2. These compounds show greatly enhanced activity in isolated plasma. Selected derivatives such as compounds 51 and 52 are orally active with a good duration of action.
从两个相关的2-（烷硫基）-嘧啶酮系列出发，设计了一系列新型的1-（（酰胺连接的）烷基）-嘧啶酮作为人脂蛋白相关磷脂酶A2的纳摩尔抑制剂。这些化合物在分离血浆中显示出大大增强的活性。所选衍生物如化合物51和52具有口服活性且作用持续时间良好。
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