Cargando…

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

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 t...

Descripción completa

Detalles Bibliográficos
Autores principales: Hayun, Hudiyono, Sumi, Hanafi, Muhammad, Yanuar, Arry
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3816667/
https://www.ncbi.nlm.nih.gov/pubmed/24281337
http://dx.doi.org/10.3390/ph5121282
_version_ 1782477969322672128
author Hayun,
Hudiyono, Sumi
Hanafi, Muhammad
Yanuar, Arry
author_facet Hayun,
Hudiyono, Sumi
Hanafi, Muhammad
Yanuar, Arry
author_sort Hayun,
collection PubMed
description 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, (1)H-NMR, (13)C-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.
format Online
Article
Text
id pubmed-3816667
institution National Center for Biotechnology Information
language English
publishDate 2012
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-38166672013-11-14 Synthesis and COX-2 Inhibitory Activity of 4-[(E)-2-(4-Oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamideand Its Analogs Hayun, Hudiyono, Sumi Hanafi, Muhammad Yanuar, Arry Pharmaceuticals (Basel) Article 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, (1)H-NMR, (13)C-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. MDPI 2012-11-27 /pmc/articles/PMC3816667/ /pubmed/24281337 http://dx.doi.org/10.3390/ph5121282 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Hayun,
Hudiyono, Sumi
Hanafi, Muhammad
Yanuar, Arry
Synthesis and COX-2 Inhibitory Activity of 4-[(E)-2-(4-Oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamideand Its Analogs
title Synthesis and COX-2 Inhibitory Activity of 4-[(E)-2-(4-Oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamideand Its Analogs
title_full Synthesis and COX-2 Inhibitory Activity of 4-[(E)-2-(4-Oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamideand Its Analogs
title_fullStr Synthesis and COX-2 Inhibitory Activity of 4-[(E)-2-(4-Oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamideand Its Analogs
title_full_unstemmed Synthesis and COX-2 Inhibitory Activity of 4-[(E)-2-(4-Oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamideand Its Analogs
title_short Synthesis and COX-2 Inhibitory Activity of 4-[(E)-2-(4-Oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamideand Its Analogs
title_sort synthesis and cox-2 inhibitory activity of 4-[(e)-2-(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)ethenyl]benzene-1-sulfonamideand its analogs
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3816667/
https://www.ncbi.nlm.nih.gov/pubmed/24281337
http://dx.doi.org/10.3390/ph5121282
work_keys_str_mv AT hayun synthesisandcox2inhibitoryactivityof4e24oxo3phenyl34dihydroquinazolin2ylethenylbenzene1sulfonamideanditsanalogs
AT hudiyonosumi synthesisandcox2inhibitoryactivityof4e24oxo3phenyl34dihydroquinazolin2ylethenylbenzene1sulfonamideanditsanalogs
AT hanafimuhammad synthesisandcox2inhibitoryactivityof4e24oxo3phenyl34dihydroquinazolin2ylethenylbenzene1sulfonamideanditsanalogs
AT yanuararry synthesisandcox2inhibitoryactivityof4e24oxo3phenyl34dihydroquinazolin2ylethenylbenzene1sulfonamideanditsanalogs