N-1 substituted pyrimidin-4-ones:: Novel, orally active inhibitors of lipoprotein-associated phospholipase A2

被引：28

作者：

Boyd, HF ^{[1
]}

Fell, SCM ^{[1
]}

Flynn, ST ^{[1
]}

Hickey, DMB ^{[1
]}

Ife, RJ ^{[1
]}

Leach, CA ^{[1
]}

Macphee, CH ^{[1
]}

Milliner, KJ ^{[1
]}

Moores, KE ^{[1
]}

Pinto, IL ^{[1
]}

Porter, RA ^{[1
]}

Rawlings, DA ^{[1
]}

Smith, SA ^{[1
]}

Stansfield, IG ^{[1
]}

Tew, DG ^{[1
]}

Theobald, CJ ^{[1
]}

Whittaker, CM ^{[1
]}

机构：

[1] SmithKline Beecham Pharmaceut, Harlow CM19 5AW, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(00)00510-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 phopholipase A(2). 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. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2557 / 2561

页数：5

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