Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system

被引：103

作者：

Harrak, Y.

Rosell, G.

Daidone, G.

Plescia, S.

Schillaci, D.

Pujol, M. D.

机构：

[1] Univ Barcelona, Fac Farm, CSIC, Unit Assoc,Lab Quim Farmaceut, E-08028 Barcelona, Spain

[2] Univ Palermo, Fac Farm, Dipartimento Chim & Tecnol Farmaceut, I-3290123 Palermo, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 14期

关键词：

anti-inflammatory activity; carboxylic acids; 1,4-benzodioxine; pyrrole derivatives; AINEs;

D O I：

10.1016/j.bmc.2007.04.050

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

A series of substituted derivatives containing the 1,4-benzodioxine or pyrrole nucleus are described. All the newly synthesized compounds were examined for their in vitro and in vivo anti-inflammatory activity. Several derivatives, including (S)-2, 14 and 17, showed more anti-inflammatory activity in vivo in these assays (rat paw oedema induced by carrageenan) than the known classical anti-inflammatory agent ibuprofen, whereas other compounds like 1 were equipotent to ibuprofen. Compound 17 was the most outstanding derivative because of its remarkable in vivo anti-inflammatory activity. In this paper, we examine and discuss the structure-activity relationships and anti-inflammatory activities of these compounds. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：4876 / 4890

页数：15

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