2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2

被引：17

作者：

Boyd, HF ^{[1
]}

Flynn, ST ^{[1
]}

Hickey, DMB ^{[1
]}

Ife, RJ ^{[1
]}

Jones, M ^{[1
]}

Leach, CA ^{[1
]}

Macphee, CH ^{[1
]}

Milliner, KJ ^{[1
]}

Rawlings, DA ^{[1
]}

Slingsby, BP ^{[1
]}

Smith, SA ^{[1
]}

Stansfield, IG ^{[1
]}

Tew, DG ^{[1
]}

Theobald, CJ ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(00)00002-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from two weakly active hits from high throughput screening, a novel series of 2-(alkylthio)-pyrimidin-4-ones with high potency and selectivity for lipoprotein-associated phospholipase Az has been designed. In contrast to previously known inhibitors, these have been shown to act by a non-covalent and substrate competitive mechanism. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：395 / 398

页数：4

共 9 条

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