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
1
Faculty of Pharmacy, University of Indonesia, Depok 16424, West Java, Indonesia
2
Department of Chemistry, Faculty of Natural Sciences, University of Indonesia, Depok 16424, West Java, Indonesia
3
Research Center for Chemistry, Indonesian Institute of Sciences, Serpong 15314, West Java, Indonesia
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2012, 5(12), 1282-1290; https://doi.org/10.3390/ph5121282
Received: 11 October 2012 / Revised: 14 November 2012 / Accepted: 23 November 2012 / Published: 27 November 2012
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.
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Keywords:
quinazolin-4-one; benzenesulfonamide; COX-2 inhibitor
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MDPI and ACS Style
Hayun; Hudiyono, S.; Hanafi, M.; Yanuar, A. 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 2012, 5, 1282-1290.
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