The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2

被引：9

作者：

Boyd, HF ^{[1
]}

Hammond, B ^{[1
]}

Hickey, DMB ^{[1
]}

Ife, RJ ^{[1
]}

Leach, CA ^{[1
]}

Lewis, VA ^{[1
]}

Macphee, CH ^{[1
]}

Milliner, KJ ^{[1
]}

Pinto, IL ^{[1
]}

Smith, SA ^{[1
]}

Stansfield, IG ^{[1
]}

Theobald, CJ ^{[1
]}

Whittaker, CM ^{[1
]}

机构：

[1] GlaxoSmithKline Pharmaceut, Harlow CM19 5AW, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(01)00038-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Modification of the pyrimidone 5-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, lipophilic inhibitors of lipoprotein-associated phospholipase A(2), has given inhibitors of nanomolar potency and improved physicochemical properties. Compound 23 was identified as a potent, highly water soluble, CNS penetrant inhibitor suitable for intravenous administration. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：701 / 704

页数：4

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