Soluble Steroids II: Amino acid derivatives

A series of amino acid derivatives of cholesterol, 9α-fluorohydrocortisone, 6α-fluoro-16α-hydroxycortisone-16,17-acetonide, and 2α-methyl-5α-dihydrotestosterone have been synthesized in a further attempt to provide compounds with increased aqueous solubility. The acylable hydroxy group of the steroi...

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Veröffentlicht in:Journal of pharmaceutical sciences 1964-04, Vol.53 (4), p.435-437
Hauptverfasser: Lange, Winthrop E., Stein, Martin E.
Format: Artikel
Sprache:eng
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Zusammenfassung:A series of amino acid derivatives of cholesterol, 9α-fluorohydrocortisone, 6α-fluoro-16α-hydroxycortisone-16,17-acetonide, and 2α-methyl-5α-dihydrotestosterone have been synthesized in a further attempt to provide compounds with increased aqueous solubility. The acylable hydroxy group of the steroid was converted to the chloroformate and was then condensed with the appropriate amino acid. The potassium salts of the various derivatives which have been prepared possess 100–600 times the aqueous solubility of the parent compounds. Infrared characteristics of the several compounds have been determined. Pharmacological studies have been undertaken and show, in general, reduced activity when the derivatives are administered subcutaneously.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600530421