Abstract
The synthesis and the in vitro pharmacological evaluation of a number of topical corticosteroid derivatives designed on the basis of the antedrug concept are reported. Three series of compounds were synthesized in which sulfur-containing amino acids were incorporated to the steroidal structure in the 21 position. Compounds of series 1 are diesters of cystine with the 21-hydroxyl groups of the corticosteroids, while series II and III contain 21-amino and 21-thio corticosteroid derivatives, respectively. The new compounds were less potent than the parent corticosteroids in vitro. The 21-yl-[9α-fluoro-11β, 17α-dihydroxy-16α-methyl-1,4-pregnadiene-3,20-dione]-S-acetylamino cysteine 13 was the most interesting compound of the series and is now under further evaluation.
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