18-Substituted steroids. Part 18. Chemical synthesis and mineralocorticoid activity of 2 alpha- and 2 beta-hydroxyaldosterone.
The 2 alpha-hydroxy and 2 beta-hydroxy derivatives of aldosterone have been synthesized chemically from aldosterone, after the earlier identification of 2 alpha-hydroxylated metabolites formed in liver. Both 2 alpha- and 2 beta-hydroxyaldosterone are potent mineralocorticoids, with activities on the order of 1/10 that of aldosterone on the basis of a rat bioassay.
Kirk
D N
DN
Department of Chemistry, Queen Mary and Westfield College, London, UK.
Schröder
M H
MH
Latif
S A
SA
Souness
G W
GW
Morris
D J
DJ
D000450:Aldosterone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D001681:Biological Assay; D004305:Dose-Response Relationship, Drug; D006900:Hydroxylation; D008297:Male; D015394:Molecular Structure; D009318:Natriuresis / Q000187:drug effects; D011188:Potassium / Q000652:urine; D051381:Rats; D017207:Rats, Sprague-Dawley
C081016:2-hydroxyaldosterone; D000450:Aldosterone; D011188:Potassium