LSteroidal Mineralocorticoid Receptor Antagonists: Synthesis and Biology

Christopher Yarnold, J. Marie Bainbridge, Helen S. Boehm,Mark Brewer,Stephen Courtney, Herve Deboves,Raffaella Di Lucrezia, Paul Giles,Estelle Hamelin, Joern Jungmann,Amedeo Leonardi,Mirco Meniconi,Carlo Riva,Andreas Scheel, Suganthan Selvaratnam, Sakthi Shanmugathasan, Giorgio Sironi, Paolo Tavecchia, David Willows

CHEMISTRYSELECT（2017）

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摘要

The development of selective steroidal mineralocorticoid receptor antagonists with improved pharmacological profiles over existing marketed drugs is an attractive goal. Such compounds offer potential for the treatment of hypertension, heart failure and renal disease. With this aim, new spirolactones were prepared exploring substitutions at carbons 6, 7, 9- 11, 15- 16 and 21. Spirolactones 11 a and 20 were identified with promising biological profiles. Both compounds restored Na+/K+ ratios to physiological levels in an in vivo model

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关键词

Antagonist,Medicinal Chemistry,Mineralocorticoid Receptor,Spirolactones,Steroids

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