2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists

被引：12

作者：

Andres, Miriam ^{[1
]}

Bravo, Monica ^{[1
]}

Antonia Buil, Maria ^{[1
]}

Calbet, Marta ^{[1
]}

Castillo, Marcos ^{[2
]}

Castro, Jordi ^{[1
]}

Eichhorn, Peter ^{[1
]}

Ferrer, Manel ^{[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

[2] Almirall Barcelona Sci Pk Unit, Barcelona 08028, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 71卷

关键词：

Pyrazole; CRTh2; antagonists; Structure-activity relationship (SAR); PROSTAGLANDIN D-2 RECEPTOR; PLASMA-PROTEIN; CUTTING EDGE; CELLS; ACTIVATION; ALKYLATION; BINDING; RAT;

D O I：

10.1016/j.ejmech.2013.10.072

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this manuscript, the synthesis and biological activity of a series of pyrazole acetic acid derivatives as CRTh2 antagonists is presented. Biological evaluation in vitro revealed that the pyrazole core showed in several cases a different structure activity relationship (SAR) to that of related indole acetic acid. A potent series of ortho-sulfonyl benzyl substituents was found, from which compounds 27 and 63 were advanced to in vivo profiling. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：168 / 184

页数：17

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