Discovery of a Potent and Orally Bioavailable CCR2 and CCR5 Dual Antagonist

被引：34

作者：

Pasternak, Alexander ^{[1
]}

Goble, Stephen D. ^{[1
]}

Struthers, Mary ^{[1
]}

Vicario, Pasquale P. ^{[1
]}

Ayala, Julia M. ^{[1
]}

Di Salvo, Jerry ^{[1
]}

Kilburn, Ruth ^{[1
]}

Wisniewski, Thomas ^{[1
]}

DeMartino, Julie A. ^{[1
]}

Mills, Sander G. ^{[1
]}

Yang, Lihu ^{[1
]}

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2010年 / 1卷 / 01期

关键词：

CCR2; CCR5; chemokine; dual antagonist; RHEUMATOID-ARTHRITIS; DOUBLE-BLIND; RECEPTOR; DISEASE; MICE;

D O I：

10.1021/ml900009d

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This report describes the discovery of a potent, orally bioavailable CC chemokine receptor 2 (CCR2) antagonist which, while optimized for CCR2 potency, also had potent CC chemokine receptor 5 (CCR5) activity

引用

页码：14 / 18

页数：5

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