Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors

New series of 3,4-diaryl-2-thioxoimidazolidin-4-ones and 3-alkylthio-4,5-diaryl-4H-1,2,4-triazoles were designed, synthesized and evaluated for their activity as anti-inflammatory agents. Compounds 20, 21, 23 and 34 are highly selective inhibitors of COX-2 enzyme at a concentration of 100 mM relativ...

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Detalles Bibliográficos
Autores principales: Al-Turki, Deema A., Al-Omar, Mohamed A., Abou-zeid, Laila A., Shehata, Ihsan A., Al-Awady, Mohammed S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2017
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5310148/
https://www.ncbi.nlm.nih.gov/pubmed/28223863
http://dx.doi.org/10.1016/j.jsps.2015.07.001
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author Al-Turki, Deema A.
Al-Omar, Mohamed A.
Abou-zeid, Laila A.
Shehata, Ihsan A.
Al-Awady, Mohammed S.
author_facet Al-Turki, Deema A.
Al-Omar, Mohamed A.
Abou-zeid, Laila A.
Shehata, Ihsan A.
Al-Awady, Mohammed S.
author_sort Al-Turki, Deema A.
collection PubMed
description New series of 3,4-diaryl-2-thioxoimidazolidin-4-ones and 3-alkylthio-4,5-diaryl-4H-1,2,4-triazoles were designed, synthesized and evaluated for their activity as anti-inflammatory agents. Compounds 20, 21, 23 and 34 are highly selective inhibitors of COX-2 enzyme at a concentration of 100 mM relative to celecoxib, the standard reference. (±)-3-(4-Phenoxy-phenyl)-5-phenyl-2-thioxoimidazolidin-4-ones 23 exhibited the most active anti-inflammatory agent.
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spelling pubmed-53101482017-02-21 Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors Al-Turki, Deema A. Al-Omar, Mohamed A. Abou-zeid, Laila A. Shehata, Ihsan A. Al-Awady, Mohammed S. Saudi Pharm J Original Article New series of 3,4-diaryl-2-thioxoimidazolidin-4-ones and 3-alkylthio-4,5-diaryl-4H-1,2,4-triazoles were designed, synthesized and evaluated for their activity as anti-inflammatory agents. Compounds 20, 21, 23 and 34 are highly selective inhibitors of COX-2 enzyme at a concentration of 100 mM relative to celecoxib, the standard reference. (±)-3-(4-Phenoxy-phenyl)-5-phenyl-2-thioxoimidazolidin-4-ones 23 exhibited the most active anti-inflammatory agent. Elsevier 2017-01 2015-07-26 /pmc/articles/PMC5310148/ /pubmed/28223863 http://dx.doi.org/10.1016/j.jsps.2015.07.001 Text en © 2015 Production and hosting by Elsevier B.V. on behalf of King Saud University. https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Original Article
Al-Turki, Deema A.
Al-Omar, Mohamed A.
Abou-zeid, Laila A.
Shehata, Ihsan A.
Al-Awady, Mohammed S.
Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors
title Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors
title_full Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors
title_fullStr Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors
title_full_unstemmed Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors
title_short Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors
title_sort design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (cox-2) inhibitors
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5310148/
https://www.ncbi.nlm.nih.gov/pubmed/28223863
http://dx.doi.org/10.1016/j.jsps.2015.07.001
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