Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives

被引：151

作者：

Alafeefy, Ahmed M. ^{[1
]}

Kadi, Adnan A. ^{[1
]}

Al-Deeb, Omar A. ^{[1
]}

El-Tahir, Kamal E. H. ^{[2
]}

Al-jaber, Nabila A. ^{[3
]}

机构：

[1] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia

[2] King Saud Univ, Coll Pharm, Dept Pharmacol, Riyadh 11451, Saudi Arabia

[3] King Saud Univ, Coll Sci, Dept Chem, Riyadh 11451, Saudi Arabia

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 11期

关键词：

Quinazoline; Analgesic; Anti-inflammatory; Synthesis; NF-KAPPA-B; POTENT INHIBITORS; STRUCTURAL CLASS; ACTIVATION; AGENTS; CELLS;

D O I：

10.1016/j.ejmech.2010.07.067

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of some new 2,4,6-trisubstituted-quinazoline derivatives were prepared and screened for their analgesic, anti-inflammatory activity and acute toxicity. Four compounds were more potent analgesic agents than the reference drug Indomethacin and thirteen compounds showed significant anti-inflammatory activity. Seven compounds showed combined ability to inhibit both pain and inflammation. Compounds tested for acute toxicity showed no toxic symptoms or mortality rates 24 h post-administration implying their good safety margin. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：4947 / 4952

页数：6

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