title: Synthesis and biological acitivity of annulated pyrazoles as selective COX-2 inhibitors. I.
abstract: A series of disubstituted 4,5-polymethylenepyrazoles were synthesized and evaluated their inhibitory activities against COX-2. Some compounds showed strong (0.3 nM) inhibitory activity on COX-2 and were found somewhat selective (up to 16) on COX-2 over COX-1.
authors.affiliation: College of Pharmacy, Yeungnam University Kyongsan, Korea.
authors.forename: H H
authors.initials: HH
authors.lastname: Kim
authors.forename: J G
authors.initials: JG
authors.lastname: Park
authors.forename: T C
authors.initials: TC
authors.lastname: Moon
authors.forename: H W
authors.initials: HW
authors.lastname: Chang
authors.forename: Y
authors.initials: Y
authors.lastname: Jahng
mesh_terms: D000818:Animals; D001854:Bone Marrow Cells / Q000187:drug effects / Q000201:enzymology; D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007527:Isoenzymes / Q000378:metabolism*; D008297:Male; D008407:Mast Cells / Q000187:drug effects / Q000201:enzymology; D051379:Mice; D008807:Mice, Inbred BALB C; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism*; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D011720:Pyrazoles; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases