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

…, H Laurent, W Losert, J Casals-Stenzel…

Index: Nickisch; Bittler; Laurent; Losert; Casals-Stenzel; Nishino; Schillinger; Wiechert Journal of Medicinal Chemistry, 1987 , vol. 30, # 8 p. 1403 - 1409

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Citation Number: 22

Abstract

Some 15, 16-methylene derivatives of the aldosterone antagonist spironolactone (1) were synthesized with the purpose of increasing the antialdosterone potency and reducing the endocrinological effects of this standard compound. By introduction of a 1, a-double bond and a 15@, 16@-methylene ring in the spironolactone molecule both goals were achieved. In animal studies mespirenone (13) exhibited a threefold-greater antialdosterone potency ...