title: Design, synthesis, molecular modeling and biological evaluation of novel diaryl heterocyclic analogs as potential selective cyclooxygenase-2 (COX-2) inhibitors.
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. Compounds20,21,23and34are 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-ones23exhibited the most active anti-inflammatory agent.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, P.O. Box 2457, King Saud University, Riyadh 11451, Saudi Arabia.
authors.forename: Deema A
authors.initials: DA
authors.lastname: Al-Turki
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, P.O. Box 2457, King Saud University, Riyadh 11451, Saudi Arabia.
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Al-Omar
authors.affiliation: Department of Organic Pharmaceutical Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
authors.forename: Laila A
authors.initials: LA
authors.lastname: Abou-Zeid
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
authors.forename: Ihsan A
authors.initials: IA
authors.lastname: Shehata
authors.affiliation: Department of Pharmacology, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
authors.forename: Mohammed S
authors.initials: MS
authors.lastname: Al-Awady
keywords: Anti-inflammatory; Docking; Selective COX-2 inhibitors; Synthesis