Hit-to-lead studies: The discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists

被引：46

作者：

Baxter, A ^{[1
]}

Cooper, A ^{[1
]}

Kinchin, E ^{[1
]}

Moakes, K ^{[1
]}

Unitt, J ^{[1
]}

Wallace, A ^{[1
]}

机构：

[1] AstraZeneca R&D Charnwood, Loughborough LE11 5RH, Leics, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 04期

关键词：

CXCR2; antagonist; hit-to-lead;

D O I：

10.1016/j.bmcl.2005.10.091

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A Hit-to-Lead optimisation programme was carried out on a high throughput screening hit, the thiazolopyrimidine 1, resulting in the discovery of the potent, orally bioavailable CXCR2 antagonist 29. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：960 / 963

页数：4

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