Potent, orally active inhibitors of lipoprotein-associated phospholipase A2:: 1-(biphenylmethylamidoalkyl)-pyrimidones

被引：28

作者：

Boyd, HF ^{[1
]}

Fell, SCM ^{[1
]}

Hickey, DMB ^{[1
]}

Ife, RJ ^{[1
]}

Leach, CA ^{[1
]}

Macphee, CH ^{[1
]}

Milliner, KJ ^{[1
]}

Pinto, IL ^{[1
]}

Rawlings, DA ^{[1
]}

Smith, SA ^{[1
]}

Stansfield, IG ^{[1
]}

Stanway, SJ ^{[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 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)00678-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1-(biphenylmethylamidoalkyl)-pyrimidones has been designed as nanomolar inhibitors of recombinant lipoprotein-associated phospholipase A(2) with high potency in whole human plasma. 5-(Pyrazolylmethyl) derivative 16 and 5-(methoxypyrimidinylmethyl) derivative 27 demonstrated excellent pharmacodynamic profiles which correlated well with their pharmacokinetic effects. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：51 / 55

页数：5

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