1,3-Diarylcycloalkanopyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2

Novel 1,3-diarylcycloalkanopyrazoles 1, and diphenyl hydrazides 2 were identified as selective inhibitors of cyclooxygenase-2. The 1,3-diaryl substitution pattern of the pyrazole ring in 1 differentiates these compounds from most of the known selective COX-2 inhibitors that contain two aryl rings at...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-03, Vol.10 (6), p.601-604
Main Authors: ZHIHUA SUI, JIHUA GUAN, FERRO, M. P, MCCOY, K, WACHTER, M. P, MURRAY, W. V, SINGER, M, STEBER, M, RITCHIE, D. M, ARGENTIERI, D. C
Format: Article
Language:English
Subjects:
Azides - chemical synthesis
Azides - pharmacology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cyclooxygenase 1
Cyclooxygenase 2
Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors - chemical synthesis
Cyclooxygenase Inhibitors - pharmacology
Humans
Isoenzymes - drug effects
Medical sciences
Membrane Proteins
Pharmacology. Drug treatments
Prostaglandin-Endoperoxide Synthases - drug effects
Pyrazoles - chemical synthesis
Pyrazoles - pharmacology
Structure-Activity Relationship
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Summary:Novel 1,3-diarylcycloalkanopyrazoles 1, and diphenyl hydrazides 2 were identified as selective inhibitors of cyclooxygenase-2. The 1,3-diaryl substitution pattern of the pyrazole ring in 1 differentiates these compounds from most of the known selective COX-2 inhibitors that contain two aryl rings at the adjacent positions on a heterocyclic or a phenyl ring. Similarly, the two phenyl rings in 2 are also separated by three atoms. SAR of both phenyl rings in 1 and 2, and the aliphatic ring in 1 will be discussed.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00041-X