Synthesis and COX-2 Inhibitory Activity of 4-[(E)-2-(4-Oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamide and Its Analogs

被引：6
|
作者：
Hayun [1 ]
Hudiyono, Sumi [2 ]
Hanafi, Muhammad [3 ]
Yanuar, Arry [1 ]
机构：
[1] Univ Indonesia, Fac Pharm, Depok 16424, West Java, Indonesia
[2] Univ Indonesia, Fac Nat Sci, Dept Chem, Depok 16424, West Java, Indonesia
[3] Indonesian Inst Sci, Res Ctr Chem, Serpong 15314, West Java, Indonesia
来源：
PHARMACEUTICALS | 2012年 / 5卷 / 12期
关键词：
quinazolin-4-one; benzenesulfonamide; COX-2; inhibitor;
D O I：
10.3390/ph5121282
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Some novel 3-phenyl-2-[(E)-2-phenylethenyl]-3,4-dihydroquinazolin-4-one derivatives possessing para-sulfonamides groups on the phenyl ring of the 2-phenylethenyl moiety have been synthesized and their COX-2 inhibitory activity evaluated. The stuctures of the synthesized compounds were confirmed on the basis of FT-IR, H-1-NMR, C-13-NMR and mass spectral data. The COX-2 inhibition screening assay revealed that 4-[(E)-2-{3-(4-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl}ethenyl]benzene-1-sulfonamide had a maximum COX-2 inhibition (47.1%), at a concentration of 20 mu M.
引用
收藏
页码：1282 / 1290
页数：9
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