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

Pharmaceuticals

rib-type="author">Hayun1*Hayun³  Sumi Hudiyono¹  Muhammad Hanafi² 

[1] Department of Chemistry, Faculty of Natural Sciences, University of Indonesia, Depok 16424, West Java, Indonesia;Research Center for Chemistry, Indonesian Institute of Sciences, Serpong 15314, West Java, Indonesia;Faculty of Pharmacy, University of Indonesia, Depok 16424, West Java, Indonesia;

关键词: quinazolin-4-one;    benzenesulfonamide;    COX-2 inhibitor;   

DOI  :  10.3390/ph5121282

来源: mdpi

【 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, ¹H-NMR, ¹³C-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 μM.

【 授权许可】

CC BY   
© 2012 by the authors; licensee MDPI, Basel, Switzerland.