17α-炔基-11β,17-二羟基雄甾烷衍生物：一类新型强效糖皮质激素。
17 alpha-alkynyl-11 beta, 17-dihydroxyandrostane derivatives : a new class of potent glucocorticoids.
作者信息
Teutsch G, Costerousse G, Deraedt R, Benzoni J, Fortin M, Philibert D
出版信息
Steroids. 1981 Dec;38(6):651-65. doi: 10.1016/0039-128x(81)90084-2.
PMID:7336464
Abstract
Replacement of the characteristic dihydroxyacetone side chain of corticoids by a 17 alpha-alkynyl-17 beta-hydroxy moiety was investigated. It was found that, in particular, the 17 alpha-propynyl substitution is favorable for high local anti-inflammatory activity with reduced systemic effects. Moreover, these compounds were found to be devoid of any affinity for the aldosterone receptor, and may thus be considered as pure glucocorticoids.
摘要
研究了用17α-炔基-17β-羟基部分取代皮质激素特有的二羟基丙酮侧链的情况。结果发现，特别是17α-丙炔基取代有利于获得高局部抗炎活性且全身作用减弱。此外，发现这些化合物对醛固酮受体没有任何亲和力，因此可被视为纯糖皮质激素。
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