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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| Format: | Article |
| Language: | English |
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Elsevier
2017-01-01
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| Series: | Saudi Pharmaceutical Journal |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016415001243 |
| _version_ | 1819267780700012544 |
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| author | Deema A. Al-Turki Mohamed A. Al-Omar Laila A. Abou-zeid Ihsan A. Shehata Mohammed S. Al-Awady |
| author_facet | Deema A. Al-Turki Mohamed A. Al-Omar Laila A. Abou-zeid Ihsan A. Shehata Mohammed S. Al-Awady |
| author_sort | Deema A. Al-Turki |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-12-23T21:22:37Z |
| format | Article |
| id | doaj.art-5470c91bbe4e4951baf1c295588ddf1a |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-12-23T21:22:37Z |
| publishDate | 2017-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-5470c91bbe4e4951baf1c295588ddf1a2022-12-21T17:30:42ZengElsevierSaudi Pharmaceutical Journal1319-01642017-01-01251596910.1016/j.jsps.2015.07.001Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitorsDeema A. Al-Turki0Mohamed A. Al-Omar1Laila A. Abou-zeid2Ihsan A. Shehata3Mohammed S. Al-Awady4Department of Pharmaceutical Chemistry, College of Pharmacy, P.O. Box 2457, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, P.O. Box 2457, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Organic Pharmaceutical Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptDepartment of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptDepartment of Pharmacology, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptNew 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.http://www.sciencedirect.com/science/article/pii/S1319016415001243Selective COX-2 inhibitorsDockingSynthesisAnti-inflammatory |
| spellingShingle | Deema A. Al-Turki Mohamed A. Al-Omar Laila A. Abou-zeid Ihsan A. Shehata Mohammed S. Al-Awady Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors Saudi Pharmaceutical Journal Selective COX-2 inhibitors Docking Synthesis Anti-inflammatory |
| 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 | Selective COX-2 inhibitors Docking Synthesis Anti-inflammatory |
| url | http://www.sciencedirect.com/science/article/pii/S1319016415001243 |
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