Aldosterone antagonists. 2. New 7 alpha-(acetylthio)-15,16-methylene spirolactones.

Basic Information

ID: ALA1123807

Journal: J Med Chem

Title: Aldosterone antagonists. 2. New 7 alpha-(acetylthio)-15,16-methylene spirolactones.

Authors: Nickisch K, Bittler D, Laurent H, Losert W, Casals-Stenzel J, Nishino Y, Schillinger E, Wiechert R.

Abstract: Some 15,16-methylene derivatives of the aldosterone antagonist spironolactone were synthesized with the purpose of increasing the antialdosterone potency and reducing the endocrinological effects of this standard compound. By introduction of a 1,2-double bond and a 15 beta,16 beta-methylene ring in the spironolactone molecule both goals were achieved. In animal studies mespirenone exhibited a threefold-greater antialdosterone potency and less than 10% of the antiandrogenic activity of spironolactone.

CiteXplore: 3612688

DOI: 10.1021/jm00391a023

Patent ID: