Synthesis and biological acitivity of annulated pyrazoles as selective COX-2 inhibitors. I.
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.
Kim
H H
HH
College of Pharmacy, Yeungnam University Kyongsan, Korea.
Park
J G
JG
Moon
T C
TC
Chang
H W
HW
Jahng
Y
Y
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
D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D011720:Pyrazoles; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases