Synthesis and biological acitivity of annulated pyrazoles as selective COX-2 inhibitors. I

H H Kim; J G Park; T C Moon; H W Chang; Y Jahng

doi:10.1007/BF02979060

Synthesis and biological acitivity of annulated pyrazoles as selective COX-2 inhibitors. I

Arch Pharm Res. 1999 Aug;22(4):372-9. doi: 10.1007/BF02979060.

Authors

H H Kim¹, J G Park, T C Moon, H W Chang, Y Jahng

Affiliation

¹ College of Pharmacy, Yeungnam University Kyongsan, Korea.

PMID: 10489876
DOI: 10.1007/BF02979060

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Bone Marrow Cells / drug effects
Bone Marrow Cells / enzymology
Cyclooxygenase 2
Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors / chemical synthesis*
Cyclooxygenase Inhibitors / pharmacology*
Isoenzymes / metabolism*
Male
Mast Cells / drug effects
Mast Cells / enzymology
Mice
Mice, Inbred BALB C
Prostaglandin-Endoperoxide Synthases / metabolism*
Pyrazoles / chemical synthesis*
Pyrazoles / pharmacology*
Structure-Activity Relationship

Substances

Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors
Isoenzymes
Pyrazoles
Cyclooxygenase 2
Prostaglandin-Endoperoxide Synthases