Steroidal Mineralocorticoid Receptor Antagonists: Synthesis and Biology
| Autor: | Stephen Martin Courtney, Suganthan Selvaratnam, Christopher John Yarnold, Paolo Tavecchia, Mirco Meniconi, Carlo Riva, Estelle M. N. Hamelin, Helen S. Boehm, Raffaella Di Lucrezia, David Willows, Paul Giles, J. Marie Bainbridge, Jörn Jungmann, Sakthi Shanmugathasan, Hervé Deboves, Giorgio Sironi, Amedeo Leonardi, Mark Brewer, Andreas Scheel |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
medicine.medical_specialty Chemistry Antagonist General Chemistry Pharmacology medicine.disease 01 natural sciences 0104 chemical sciences 010404 medicinal & biomolecular chemistry 03 medical and health sciences 030104 developmental biology Mineralocorticoid receptor Endocrinology Heart failure Internal medicine medicine |
| Zdroj: | ChemistrySelect. 2:175-189 |
| ISSN: | 2365-6549 |
| Popis: | 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 |
| Databáze: | OpenAIRE |
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