The identification of clinical candidate SB-480848:: A potent inhibitor of lipoprotein-associated phospholipase A2

被引：103

作者：

Blackie, JA ^{[1
]}

Bloomer, JC ^{[1
]}

Brown, MJB ^{[1
]}

Cheng, HY ^{[1
]}

Hammond, B ^{[1
]}

Hickey, DMB ^{[1
]}

Ife, RJ ^{[1
]}

Leach, CA ^{[1
]}

Lewis, VA ^{[1
]}

Macphee, CH ^{[1
]}

Milliner, KJ ^{[1
]}

Moores, KE ^{[1
]}

Pinto, IL ^{[1
]}

Smith, SA ^{[1
]}

Stansfield, IG ^{[1
]}

Stanway, SJ ^{[1
]}

Taylor, MA ^{[1
]}

Theobald, CJ ^{[1
]}

机构：

[1] GlaxoSmithKline, Med Res Ctr, Stevenage SG1 2NY, Herts, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(03)00058-1

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 clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency. Cyclopentyl fused derivative 21, SB-480848, showed an enhanced in vitro and in vivo profile versus SB-435495 and has been selected for progression to man. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1067 / 1070

页数：4

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