2-(1H-Pyrazol-4-yl) acetic acids as CRTh2 antagonists

被引：11

作者：

Andres, Miriam ^{[1
]}

Bravo, Monica ^{[1
]}

Antonia Buil, Maria ^{[1
]}

Calbet, Marta ^{[1
]}

Castro, Jordi ^{[1
]}

Domenech, Teresa ^{[1
]}

Eichhorn, Peter ^{[1
]}

Ferrer, Manel ^{[1
]}

Gomez, Elena ^{[1
]}

Lehner, Martin D. ^{[1
]}

Moreno, Imma ^{[1
]}

Roberts, Richard S. ^{[1
]}

Sevilla, Sara ^{[1
]}

机构：

[1] Almirall R&D Ctr, Barcelona 08980, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 11期

关键词：

CRTh2; Prostaglandin D2; Antagonist; Pyrazole; Plasma protein binding; PROSTAGLANDIN D-2 RECEPTOR; HELPER TYPE-2 CELLS; HUMAN TH2 CELLS; PLASMA-PROTEIN; CUTTING EDGE; MOLECULE; ACTIVATION; POTENT; DISCOVERY; BINDING;

D O I：

10.1016/j.bmcl.2013.03.093

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

High throughput screening identified the pyrazole-4-acetic acid substructure as CRTh2 receptor antagonists. Optimisation of the compounds uncovered a tight SAR but also identified some low nanomolar inhibitors. (C) 2013 Elsevier Ltd. All rights reserved.

引用

收藏

页码：3349 / 3353

页数：5

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