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  • Title: Aldosterone antagonists. 2. New 7 alpha-(acetylthio)-15,16-methylene spirolactones.
    Author: Nickisch K, Bittler D, Laurent H, Losert W, Casals-Stenzel J, Nishino Y, Schillinger E, Wiechert R.
    Journal: J Med Chem; 1987 Aug; 30(8):1403-9. PubMed ID: 3612688.
    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.
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