Selective effects of 7 alpha-halogeno substitution on corticosteroid activity: Sch 22219 and Sch 23409.
Two 7 alpha-halogeno substituted corticosteroids, 7 alpha-chloro-16 alpha-methylprednisolone-17,21 dipropionate (Sch 22219) and 7 alpha-bromo-16 alpha-methylprednisolone-17-benzoate-21-acetate (Sch 23409) were compared to other clinically utilized topical corticosteroids for local and parenteral antiinflammatory and glucocorticosteroid activity. Both compounds were at least equivalent to the most potent comparison corticosteroids in topical antiinflammatory activity, and exhibited favorable ratios of local to systemic effects. In mice, Sch 22219 showed a greater dissociation of antiinflammatory activity from side effects than Sch 23409, although the reverse was true in rats. On the basis of the data available, both compounds possess enhanced topical antiinflammatory potency, with the potential for reduced side effects in man.
D000311:Adrenal Glands / Q000187:drug effects; D000818:Animals; D001284:Atrophy / Q000139:chemically induced; D003436:Croton Oil / Q000037:antagonists & inhibitors; D004431:Ear, External / Q000187:drug effects; D005260:Female; D005938:Glucocorticoids / Q000494:pharmacology; D008297:Male; D008775:Methylprednisolone / Q000494:pharmacology*; D051381:Rats; D012871:Skin Diseases / Q000139:chemically induced; D013329:Structure-Activity Relationship
D005938:Glucocorticoids; D003436:Croton Oil; D008775:Methylprednisolone