Synthesis and antimineralocorticoid activities of some 7alpha-cyano and 7alpha-alkoxycarbonylamino steroidal spirolactones

J Med Chem. 1976 Jul;19(7):975-7. doi: 10.1021/jm00229a025.

Abstract

The synthesis and antimineralocorticoid potencies of several steroidal spirolactones bearing novel nitrogenous substituents in the 7alpha position are reported. These substituents include the cyano, the isocyanato, and the alkoxycarbonylamino groupings. The nitrile 1b and the N-carbomethoxy compound 1h showed good antimineralocorticoid potency (MED less than or equal to 0.79 mg) on subcutaneous administration to adrenalectomized rats.

MeSH terms

  • Adrenal Glands / physiology
  • Adrenalectomy
  • Animals
  • Depression, Chemical
  • Desoxycorticosterone / antagonists & inhibitors
  • Electrolytes / urine
  • Mineralocorticoids / antagonists & inhibitors*
  • Pregnenes / chemical synthesis*
  • Pregnenes / pharmacology
  • Rats
  • Spiro Compounds / chemical synthesis*
  • Spiro Compounds / pharmacology

Substances

  • Electrolytes
  • Mineralocorticoids
  • Pregnenes
  • Spiro Compounds
  • Desoxycorticosterone