[Synthesis and reactions of 2-methylene-canrenone].
Starting from the Mannich salt 1 of the aldosterone antagonist canrenone or from 2-methylene-canrenone (2) the A-ring annulated hetero- and carbocycles 5, 6, 8-13 were prepared. Receptor (estradiol, progesterone, androgen, gluco- and mineralocorticoid) binding studies and competition studies with the serum proteins SHBG and CBG were carried out using the compounds 2, 3, 4b, 5, 6b, 8 and 12. The relative binding affinities with CBG are below 1%, in all other cases lower than 0.01%.
Görlitzer
K
K
Institut für Pharmazeutische Chemie, Technischen Universität Braunschweig.
Moormann
P
P
Pollow
K
K
Schaffrath
M
M
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001798:Blood Proteins / Q000378:metabolism; D002192:Canrenone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D051381:Rats; D017208:Rats, Wistar; D011956:Receptors, Cell Surface / Q000378:metabolism*
C093222:2-methylenecanrenone; D001798:Blood Proteins; D011956:Receptors, Cell Surface; D002192:Canrenone
Darstellung und Reaktionen von 2-methylen-canrenon.