1,5-diarylpyrrole-3-acetic acids and esters as novel classes of potent and highly selective cyclooxygenase-2 inhibitors

被引：53

作者：

Biava, M

Porretta, GC

Cappelli, A

Vomero, S

Manetti, F

Botta, M

Sautebin, L

Rossi, A

Makovec, F

Anzini, M

机构：

[1] Univ Roma La Sapienza, Dipartimento Studi Chim & Tecnol Sostanze Biologi, I-00185 Rome, Italy

[2] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy

[3] Univ Siena, European Res Ctr Drug Res & Dev, I-53100 Siena, Italy

[4] Univ Naples Federico II, Dipartimento Farmacol Sperimentale, I-80131 Naples, Italy

[5] Rotta Res Labs SpA, I-20052 Monza, Italy

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 09期

关键词：

D O I：

10.1021/jm049121q

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A small set of substituted 1,5-diarylpyrrole-3-acetic and -glyoxylic acid derivatives have been synthesized, and their cyclooxygenase (COX-1 and COX-2) inhibiting properties have been evaluated. Some compounds proved to be highly selective COX-2 inhibitors, and their affinity data have been rationalized through docking simulations in terms of interactions with a crystallographic model of the COX-2 binding site.

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页码：3428 / 3432

页数：5

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