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Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors
Journal article   Open access  Peer reviewed

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

Deema A. Al-Turki, Mohamed A. Al-Omar, Laila A. Abou-zeid, Ihsan A. Shehata and Mohammed S. Al-Awady
Saudi pharmaceutical journal, Vol.25(1), pp.59-69
01/01/2017
DOI: https://doi.org/10.1016/j.jsps.2015.07.001
PMCID: PMC5310148
PMID: 28223863

Abstract

Anti-inflammatory Docking Selective COX-2 inhibitors Synthesis
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 100mM 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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https://doi.org/10.1016/j.jsps.2015.07.001View
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