Prepartion of 16alpha-alkoxy and 16alpha-acyloxy derivatives of 21-chloro-17-acyloxy corticosteroids and determination of their vasoconstrictor activities in humans.
A number of number of 16alpha-alkoxy and 16alpha-acyloxy derivatives of 21-chloro-17-acyloxy corticosteroids have been prepared. The synthetic routes used were (a) reaction of the 16alpha,17-disubstituted 21-mesylate with lithium chloride and (b) reaction of the 16alpha-substituted 17,21-cyclic ortho ester with triphenylmethyl chloride. The vasoconstrictor activities in humans exhibited by these compounds were significantly lower than that of a 16beta-methyl analogue.
D001624:Betamethasone Valerate / Q000494:pharmacology; D006801:Humans; D011282:Pregnenediones / Q000138:chemical synthesis* / Q000494:pharmacology; D012867:Skin / Q000187:drug effects; D013258:Steroids, Chlorinated / Q000138:chemical synthesis / Q000494:pharmacology; D014662:Vasoconstrictor Agents / Q000138:chemical synthesis*; D014666:Vasomotor System / Q000187:drug effects
D011282:Pregnenediones; D013258:Steroids, Chlorinated; D014662:Vasoconstrictor Agents; D001624:Betamethasone Valerate