18-Substituted progesterone derivatives as inhibitors of aldosterone biosynthesis.
The synthesis of new progesterone derivatives substituted at the 18 methyl group is described. These compounds are designed as 18-monooxygenase, cytochrome P-450-dependent potential kcat inhibitors. Preliminary results on the in vitro biological investigation of these modified progesterones are presented.
Laboratoire de Chimie Organique Biologique, UA CNRS 493, Université Paris VI, France.
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Viger
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Coustal
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Perard
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Piffeteau
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Marquet
D000311:Adrenal Glands / Q000187:drug effects / Q000378:metabolism*; D000450:Aldosterone / Q000096:biosynthesis*; D000818:Animals; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D000451:Mineralocorticoid Receptor Antagonists / Q000494:pharmacology*; D011374:Progesterone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D007202:Indicators and Reagents; D000451:Mineralocorticoid Receptor Antagonists; D000450:Aldosterone; D011374:Progesterone