1,5-Diarylimidazoles with strong inhibitory activity against COX-2 catalyzed PGE2 production from LPS-induced RAW 264.7 cells.
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.
Che
Haiyan
H
College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
Tuyen
Truong Ngoc
TN
Kim
Hyun Pyo
HP
Park
Haeil
H
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
D052246:Cyclooxygenase 2 Inhibitors; D007093:Imidazoles; D008070:Lipopolysaccharides; D015232:Dinoprostone