17 alpha-alkynyl-11 beta, 17-dihydroxyandrostane derivatives : a new class of potent glucocorticoids.
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.
D000732:Androstanols / Q000138:chemical synthesis / Q000378:metabolism; D000818:Animals; D005938:Glucocorticoids / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D051379:Mice; D051381:Rats; D011987:Receptors, Steroid / Q000378:metabolism; D013329:Structure-Activity Relationship
D000732:Androstanols; D005938:Glucocorticoids; D011987:Receptors, Steroid