Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists

被引：8

作者：

Cai, Chaozhong ^{[1
]}

Kang, Fu-An ^{[1
]}

Hou, Cuifen ^{[1
]}

O'Neill, John C. ^{[1
]}

Opas, Evan ^{[1
]}

McKenney, Sandra ^{[1
]}

Johnson, Dana ^{[1
]}

Sui, Zhihua ^{[1
]}

机构：

[1] Janssen Res & Dev LLC, Spring House, PA 19477 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 01期

关键词：

CCR2; Fused bicycle ring; 1,3-Dipolar cycloaddition; CHEMOKINES; ACID;

D O I：

10.1016/j.bmcl.2012.10.069

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel CCR2 antagonists with a novel 2-aminooctahydrocyclopentalene-3a-carboxamide scaffold were designed. SAR studies led to a series of potent compounds. For example, compound 51 had a good PK profile in both dog and monkey, and exhibited excellent efficacy when dosed orally in an inflammation model in hCCR2 KI mice. In addition, an asymmetric synthesis to the core structures was developed. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：351 / 354

页数：4

共 11 条

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[2] TOTAL SYNTHESIS OF (+/-)-RETIGERANIC ACID [J].