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

被引：82
|
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 ; 081704 ;
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
收藏
页码：4876 / 4890
页数：15
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