The discovery of structurally novel CCR1 antagonists derived from a hydroxyethylene peptide isostere template

被引：18

作者：

Kath, JC ^{[1
]}

DiRico, AP ^{[1
]}

Gladue, RP ^{[1
]}

Martin, WH ^{[1
]}

McElroy, EB ^{[1
]}

Stock, IA ^{[1
]}

Tylaska, LA ^{[1
]}

Zheng, DY ^{[1
]}

机构：

[1] Pfizer Inc, Global Res & Dev, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 09期

关键词：

chemokine; CCR1;

D O I：

10.1016/j.bmcl.2004.02.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present manuscript details the discovery and early fundamental structure-activity relationship studies, involving compound 3, a novel hydroxyethylene peptide isostere derived molecule that provides micromolar inhibition of CCL3 binding to its receptor CCR1. Initial studies established this screening hit as a legitimate lead for further medicinal chemistry optimization. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2163 / 2167

页数：5

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