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酯化作用对7α-氯-和7α-溴-16α-甲基泼尼松龙局部抗炎活性的影响

The influence of esterification on the topical antiinflammatory activity of 7 alpha-chloro- and 7 alpha-bromo-16 alpha-methylprednisolones.

作者信息

Green M J, Shue H J, Tiberi R, Berkenkopf J, Fernandez X, Monahan M, Lutsky B N

出版信息

Arzneimittelforschung. 1980;30(10):1618-20.

PMID:7192095
Abstract

The effect on topical antiinflammatory potency of altering the ester functions of 7-halogenocorticosteroids was examined. Highest potencies for both 7 alpha-chloro- and 7 alpha-bromo-16 alpha-methylprednisolones were generally achieved through diesterification at the 17- and 21-positions. However, among these diesters, structure seems to be more important for topical potency than lipophilicity.

摘要

研究了改变7-卤代糖皮质激素酯功能对局部抗炎效力的影响。7α-氯-和7α-溴-16α-甲基泼尼松龙的最高效力通常是通过在17位和21位进行二酯化实现的。然而,在这些二酯中,结构对局部效力的影响似乎比亲脂性更重要。

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