Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists

被引：22

作者：

Robarge, MJ ^{[1
]}

Bom, DC ^{[1
]}

Tumey, LN ^{[1
]}

Varga, N ^{[1
]}

Gleason, E ^{[1
]}

Silver, D ^{[1
]}

Song, JP ^{[1
]}

Murphy, SM ^{[1
]}

Ekema, G ^{[1
]}

Doucette, C ^{[1
]}

Hanniford, D ^{[1
]}

Palmer, M ^{[1
]}

Pawlowski, G ^{[1
]}

Danzig, J ^{[1
]}

Loftus, M ^{[1
]}

Hunady, K ^{[1
]}

Sherf, BA ^{[1
]}

Mays, RW ^{[1
]}

Stricker-Krongrad, A ^{[1
]}

Brunden, KR ^{[1
]}

Harrington, JJ ^{[1
]}

Bennani, YL ^{[1
]}

机构：

[1] Athersys Inc, Med Chem, Cleveland, OH 44115 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 06期

关键词：

CRTH-2; prostaglandin D2; ramatroban; asthma;

D O I：

10.1016/j.bmcl.2004.12.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The chemoattractant receptor-homologous molecule expressed on T(H)2 cells (CRTH-2), also found on eosinophils and basophils, is a prostaglandin D-2 receptor involved in the recruitment of these cell types during an inflammatory response. In this report, we describe the synthesis and optimization of a ramatroban isostere that is a selective and potent antagonist of CRTH-2 which may be useful in the treatment of certain diseases. © 2004 Elsevier Ltd. All rights reserved.

引用

页码：1749 / 1753

页数：5

共 14 条

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[2] Asthma - From bronchoconstriction to airways inflammation and remodeling [J].