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Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.

Jason M Cox,Hong D Chu,Christine Yang,Hong C Shen,Zhicai Wu,Jaume Balsells,Alejandro Crespo,Patricia Brown,Beata Zamlynny,Judyann Wiltsie,Joseph Clemas,Jack Gibson,Lisa Contino,JeanMarie Lisnock,Gaochao Zhou,Margarita Garcia-Calvo,Thomas Bateman,Ling Xu,Xinchun Tong,Martin Crook,Peter Sinclair

Bioorganic & Medicinal Chemistry Letters（2014）

Cited 27|Views22
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Abstract
Novel potent and selective mineralocorticoid receptor antagonists were identified, utilizing heterocyclic amide replacements in the oxazolidinedione series. Structure–activity relationship (SAR) efforts focused on improving lipophilic ligand efficiency (LLE) while maintaining nuclear hormone receptor selectivity and reasonable pharmacokinetic profiles.
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Key words
Mineralocorticoid receptor antagonist,Hypertension,Oxazolidinedione,Lipophilic ligand efficiency
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