title: 1,5-Diarylimidazoles with strong inhibitory activity against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells.
abstract: A series of 1,5-diarylimidazoles with 4-methylsulfonylphenyl group were prepared and evaluated for the inhibitory activities against COX-2 catalyzed PGE(2) production from LPS-induced RAW 264.7 cells. Most of synthesized 1,5-diarylimidazoles exhibited strong inhibitory activities regardless of the position of the 4-methylsulfonylphenyl group. The 1,5-diarylimidazoles with a halogen atom (3c-3h, 3n-3p) gave mostly excellent inhibitory activities regardless of the position and species of the halogen atom. Whereas the 1,5-diarylimidazoles with two fluorine atoms (3k, 3l, 3r, 3s) showed rather reduced inhibitory activities.
authors.affiliation: College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
authors.forename: Haiyan
authors.initials: H
authors.lastname: Che
authors.forename: Truong Ngoc
authors.initials: TN
authors.lastname: Tuyen
authors.forename: Hyun Pyo
authors.initials: HP
authors.lastname: Kim
authors.forename: Haeil
authors.initials: H
authors.lastname: Park
mesh_terms: D000818:Animals; D002384:Catalysis; D002460:Cell Line; D052246:Cyclooxygenase 2 Inhibitors / Q000378:metabolism / Q000494:pharmacology*; D015232:Dinoprostone / Q000096:biosynthesis*; D007093:Imidazoles / Q000494:pharmacology*; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects* / Q000378:metabolism; D051379:Mice
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D007093:Imidazoles; D008070:Lipopolysaccharides; D015232:Dinoprostone