Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists

被引：24

作者：

Ho, KK

Auld, DS

Bohnstedt, AC

Conti, P

Dokter, W

Erickson, S

Feng, DM

Inglese, J

Kingsbury, C

Kultgen, SG

Liu, RQ

Masterson, CM

Ohlmeyer, M

Rong, YJ

Rooseboom, M

Roughton, A

Samama, P

Smit, MJ

Son, E

van der Louw, J

Vogel, G

Webb, M

Wijkmans, J

You, M

机构：

[1] Pharmacopeia Drug Discovery Inc, Princeton, NJ 08543 USA

[2] NV Organon, NL-5340 BH Oss, Netherlands

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

chemokine; CXCR2; pyrimidine; microsomal stability; oral bioavailability;

D O I：

10.1016/j.bmcl.2006.02.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2724 / 2728

页数：5

共 5 条

[1] Chemokine receptors in inflammation: an overview [J].