Synthesis and biological evaluation of novel imidazolone derivatives as potential COX-2 inhibitors

被引：0
作者：
Hassanein H. Hassanein
Maha M. Khalifa
Ola N. El-Samaloty
Mohamed Abd El-Rahim
Ragia A. Taha
M. F. Magda
机构：
[1] Cairo University,Pharmaceutical Chemistry Department, Faculty of Pharmacy
[2] Al-Azhar University,Pharmaceutical Chemistry Department, Faculty of Pharmacy
[3] Cairo University,Biochemistry Department, Faculty of Pharmacy
[4] Al-Azhar University (Girls),Pharmacology Department, Faculty of Pharmacy
来源：
Archives of Pharmacal Research | 2008年 / 31卷
关键词：
Oxazolones; Imidazolones; Anti-inflammatory; COX-2 inhibition;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
Three novel series of 2-(substituted phenyl)-4-(substituted arylidene)-imidazolone-5-(4H)-ones were derived from the corresponding oxazolones by condensation with different arylamines. Eleven of the synthesized compounds were selected and evaluated for their effect on carrageenan-induced rat paw edema. Compound 4b had the same efficacy as the reference standard (indomethacin), and compounds 3b, 3c, 4a, 4d and 9a showed good to excellent activities, with other compounds only weakly active. The potent compounds were evaluated for their inhibitory activities against COX-2-catalyzed PGE2 production, with 4a, 4b and 3c showing strong inhibitory activity.
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页码：562 / 568
页数：6
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