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Bioorg Med Chem Lett. 2013 Aug 1;23(15):4388-92. doi: 10.1016/j.bmcl.2013.05.077. Epub 2013 Jun 4.

Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.

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1
Department of Discovery Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA. christine_yang@merck.com

Abstract

Novel oxazolidinedione analogs were discovered as potent and selective mineralocorticoid receptor (MR) antagonists. Structure-activity relationship (SAR) studies were focused on improving the potency and microsomal stability. Selected compounds demonstrated excellent MR activity, reasonable nuclear hormone receptor selectivity, and acceptable rat pharmacokinetics.

PMID:
23777778
DOI:
10.1016/j.bmcl.2013.05.077
[Indexed for MEDLINE]
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