Substituted pyrazolo corticoids as topical antiinflammatory agents

The synthesis of a series of substituted pyrazolo corticoids is described. Of these 11beta,17alpha,21-trihydroxy-6,16alpha-dimethyl-4,6-pregnadieno[3,2-c]-2'-(4-pyridly)pyrazole (21) shows an excellent separation of systemic to local activity in the model animal test. Compound 21 exhibits high...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1975-02, Vol.18 (2), p.168-172
Main Authors: Hannah, John, Kelly, Kenneth, Patchett, Arthur A, Steelman, Sanford L, Morgan, Evan R
Format: Article
Language:English
Subjects:
Administration, Topical
Animals
Anti-Inflammatory Agents - chemical synthesis
Anti-Inflammatory Agents - therapeutic use
Dose-Response Relationship, Drug
Female
Glucocorticoids
Gossypium
Granuloma - drug therapy
Granuloma - etiology
Humans
Optical Rotation
Progestins - chemical synthesis
Pyrazoles - chemical synthesis
Pyrazoles - therapeutic use
Rats
Structure-Activity Relationship
Vasoconstrictor Agents - chemical synthesis
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Description
Summary:The synthesis of a series of substituted pyrazolo corticoids is described. Of these 11beta,17alpha,21-trihydroxy-6,16alpha-dimethyl-4,6-pregnadieno[3,2-c]-2'-(4-pyridly)pyrazole (21) shows an excellent separation of systemic to local activity in the model animal test. Compound 21 exhibits high vasoconstriction activity in human volunteers and is clinically effective in the treatment of psoriasis.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00236a012