21-Methyl-20,21-diketocorticosteroid類の抗炎症作用(第1報)11β, 17α-Dihydroxy-21-methylpregna-1,4-diene-3,20,21-trione17-Acylate類および関連化合物の抗炎症作用

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A series of 21-methyl-20,21-diketocorticosteroids (1-10), 21-methylprednisolone derivatives (11-19) and 21-hydroxymethylcorticosteroids (20-22) were tested for anti-inflammatory activity in the carrageenin edema test, carrageenin abscess test and granuloma pouch test in rats. 11β, 17α-Dihydroxy-21-methylpregna-1,4-diene-3,20,21-trione 17-acetate (1), 17-propionate (2), 17-n-butyrate (3) and 17-benzoate (4) showed potent or slightly less activity compared to that of prednisolone, while 17-deacylated compound i.e. 11β, 17α-dihydroxy-21-methylpregna-1,4-diene-3,20,21-trione (5), did not show any significant activity at the dose tested. 6α-Methylation (6) or 9α-fluorination (7) of 1 potentiated the activity of 1 but the simultaneous introduction of 9α-fluorine and 16α-methyl groups (8) into 1 failed to potentiate its activity. 21-Methylprednisolone 17-acetate (13), 17-propionate (14), 17-n-butyrate (15), 17-benzoate (16) and 21αF-acetate (17) or 21βF-acetate (18) showed potent activity, but 21-methylprednisolone per se, 21αF-ol (11) or 21βF-ol (12), did not show any significant activity at the doses tested. 21-Hydroxy-methyldexamethasone (22) showed weak anti-inflammatory activity, and 21-hydroxymethylprednisolone (20) and 21-bis (hydroxymethyl) prednisolone (21) did not have any significant activity.
社団法人日本薬学会の論文
1979-04-25