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合成和cox - 2抑制活性的4 -[(e)- 2 -(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)乙烯基]benzene-1-sulfonamide及其类似物.pdfVIP

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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合成和cox - 2抑制活性的4 -[(e)- 2 -(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)乙烯基]benzene-1-sulfonamide及其类似物.pdf

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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合成和cox - 2抑制活性的4 -[(e)- 2 -(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)乙烯基]benzene-1-sulfonamide及其类似物

Pharmaceuticals 2012, 5, 1282-1290; doi:10.3390/ph5121282 OPEN ACCESS pharmaceuticals ISSN 1424-8247 /journal/pharmaceuticals 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 Hayun 1,*, Sumi Hudiyono 2, Muhammad Hanafi 3 and Arry Yanuar 1 1 Faculty of Pharmacy, University of Indonesia, Depok 16424, West Java, Indonesia; E-Mails: hayun.ms@ui.ac.id (H.); arry.yanuar@ui.ac.id (A.Y.) 2 Department of Chemistry, Faculty of Natural Sciences, University of Indonesia, Depok 16424, West Java, Indonesia; E-Mail: hudiyono@ui.ac.id (S.H.) 3 Research Center for Chemistry, Indonesian Institute of Sciences, Serpong 15314, West Java, Indonesia; E-Mail: hanafi124@ (M.H.) * Author to whom correspondence should be addressed; E-Mail: hayun.ms@ui.ac.id Tel.: +62-21-8744738; Fax: +62-21-7863433. Received: 11 October 2012; in revised form: 14 November 2012 / Accepted: 23 November 2012 / Published: 27 November 2012 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%),