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Elsevier, Saudi Pharmaceutical Journal, 1(25), p. 59-69, 2017

DOI: 10.1016/j.jsps.2015.07.001

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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 published in 2017 by Deema A. Al Turki, Mohamed A. Al Omar, Laila A. Abou zeid, Ihsan A. Shehata, Mohammed S. Al Awady
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

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.