The discoverv of SB-435495:: A potent, orally active inhibitor of lipoprotein-associated phospholipase A2 for evaluation in man

被引：31

作者：

Blackie, JA ^{[1
]}

Bloomer, JC ^{[1
]}

Brown, MJB ^{[1
]}

Cheng, HY ^{[1
]}

Elliott, RL ^{[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
]}

Whittaker, CM ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(02)00473-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging developability properties. Diethylaminoethyl derivative 32, SB-435495, was selected for progression to man. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2603 / 2606

页数：4

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