Literature

Abstract

A series of 3-unsubstituted/substituted-4,5-diphenyl-2-oxo-3H-1,3-oxazole derivatives were prepared as selective cyclooxygenase-2 (COX-2) inhibitors. Among the synthesized compounds, 4-(4-phenyl-3-methyl-2-oxo-3H-1,3-oxazol-5-yl)benzensulfonamide (compound 6) showed selective COX-2 inhibition with a selectivity index of >50 (IC(50)COX-1=>100 microm, IC(50)COX-2=2 microm) in purified enzyme (PE) assay. Compound 6 also exhibited selective COX-2 inhibition in human whole blood assay. Molecular docking studies showed that 6 can be docked into the COX-2 binding site thus providing the molecular basis for its activity.

DOI： 10.1016/j.ejmech.2008.10.039

Synthesis and biological evaluation of 4,5-diphenyloxazolone derivatives on route towards selective COX-2 inhibitors

European Journal of Medicinal Chemistry 2009.0

4-Aryl/cycloalkyl-5-phenyloxazole derivatives as selective COX-2 inhibitors

Bioorganic & Medicinal Chemistry Letters 2002.0

Selective COX-2 inhibitors. Part 1: Synthesis and biological evaluation of phenylazobenzenesulfonamides

Bioorganic & Medicinal Chemistry Letters 2006.0

Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors

Bioorganic & Medicinal Chemistry 2010.0

Synthesis and Biological Evaluation of 3,4-Diaryloxazolones: A New Class of Orally Active Cyclooxygenase-2 Inhibitors

Journal of Medicinal Chemistry 2000.0

Design, synthesis, biological evaluation and molecular modeling of dihydropyrazole sulfonamide derivatives as potential COX-1/COX-2 inhibitors