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

被引：24

作者：

Hassanein, Hassanein H. ^{[3
]}

Maha M. Khalifa ^{[1
]}

El-Samaloty, Ola N. ^{[1
]}

El-Rahim, Mohamed Abd ^{[2
]}

Taha, Ragia A. ^{[4
]}

Magda M F Ismail ^{[1
]}

机构：

[1] Al Azhar Univ, Dept Pharmaceut Chem, Fac Pharm, Cairo 11754, Egypt

[2] Cairo Univ, Fac Pharm, Dept Biochem, Cairo, Egypt

[3] Cairo Univ, Fac Pharm, Dept Pharmaceut Chem, Al Azhar Univ, Cairo, Egypt

[4] Al Azhar Univ, Fac Pharm, Dept Pharmacol, Cairo 11754, Egypt

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2008年 / 31卷 / 05期

关键词：

oxazolones; imidazolones; anti-inflammatory; COX-2; inhibition;

D O I：

10.1007/s12272-001-1193-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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 PGE(2) production, with 4a, 4b and 3c showing strong inhibitory activity.

引用

页码：562 / 568

页数：7

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