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New steroids with antiprogestational and antiglucocorticoid activities
A number of 11-substituted 19-norsteroids with inverse configuration at C-13 were synthesized. 11 beta-Aryl compounds in this series were found to possess antiprogestational and antiglucocorticoid
Mespirenone and other 15,16-methylene-17-spirolactones, a new type of steroidal aldosterone antagonists.
The ability of a series of 15,16-methylene-spirolactones in comparison to known antimineralocorticoids to inhibit the renal actions of aldosterone was tested in adrenalectomized, glucocortioid-treated rats to obtain preliminary information on potential antiandrogenic and progestogenic (side-)effects.
New biologically active pregnan-21-oic acid esters.
Several pregnan-21-oic acid esters possess the unique activity that they are topical anti-inflammatory agents with no side effects and even when administered at high dosages, the usual systemic activity associated with corticosteroid treatment could not be observed.
Stereocontrolled derivatization of 3-methoxyestra-1,3,5(10), n-tetraenes via lewis acid promoted prins reactions, (n=7; 8(9))
Steroidal olefins 1 and 3 undergo dimethylaluminum chloride-mediated Prins reactions with paraformaldehyde to furnish homoallylic alcohols 4 and 16 as major products. These ene reaction-type
Synthesis and activities of anti-aldosterones.
The bis-methylene derivative was found to reverse the strong depression of the urinary Na/K ratio induced by the mineralocorticoid effect of aldosterone in a dose-dependent manner and had more than five times the potency of spironolactone.
Aldosterone antagonists. 2. New 7 alpha-(acetylthio)-15,16-methylene spirolactones.
In animal studies mespirenone exhibited a threefold-greater antialdosterone potency and less than 10% of the antiandrogenic activity of spironolactone.