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Pharmaceuticals 2012, 5(12), 1282-1290; doi:10.3390/ph5121282
Article

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,* , 2
,
3
 and
1
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.
Received: 11 October 2012 / Revised: 14 November 2012 / Accepted: 23 November 2012 / Published: 27 November 2012
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Abstract

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.
Keywords: quinazolin-4-one; benzenesulfonamide; COX-2 inhibitor quinazolin-4-one; benzenesulfonamide; COX-2 inhibitor
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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