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Steroidal Mineralocorticoid Receptor Antagonists: Synthesis and Biology
Author(s) -
Yarnold Christopher,
Bainbridge J. Marie,
Boehm Helen S.,
Brewer Mark,
Courtney Stephen,
Deboves Hervé,
Di Lucrezia Raffaella,
Giles Paul,
Hamelin Estelle,
Jungmann Jörn,
Leonardi Amedeo,
Meniconi Mirco,
Riva Carlo,
Scheel Andreas,
Selvaratnam Suganthan,
Shanmugathasan Sakthi,
Sironi Giorgio,
Tavecchia Paolo,
Willows David
Publication year - 2017
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201601744
Subject(s) - mineralocorticoid receptor , mineralocorticoid , in vivo , pharmacology , receptor , chemistry , endocrinology , medicine , biology , biochemistry , microbiology and biotechnology
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