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 vasoconstriction activity in human volunteers and is clinically effective in the treatment of psoriasis.
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D005260:Female; D005938:Glucocorticoids; D003368:Gossypium; D006099:Granuloma / Q000188:drug therapy / Q000209:etiology; D006801:Humans; D009904:Optical Rotation; D011372:Progestins / Q000138:chemical synthesis; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000627:therapeutic use; D051381:Rats; D013329:Structure-Activity Relationship; D014662:Vasoconstrictor Agents / Q000138:chemical synthesis
D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D011372:Progestins; D011720:Pyrazoles; D014662:Vasoconstrictor Agents