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.
Copyright © 2013 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Binding Sites
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Drug Evaluation, Preclinical
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Half-Life
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Humans
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Microsomes / metabolism
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Mineralocorticoid Receptor Antagonists / chemical synthesis
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Mineralocorticoid Receptor Antagonists / chemistry*
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Mineralocorticoid Receptor Antagonists / pharmacokinetics
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Molecular Docking Simulation
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Oxazoles / chemical synthesis
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Oxazoles / chemistry*
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Oxazoles / pharmacokinetics
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Protein Structure, Tertiary
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Rats
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Receptors, Mineralocorticoid / chemistry
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Receptors, Mineralocorticoid / metabolism*
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Structure-Activity Relationship
Substances
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Mineralocorticoid Receptor Antagonists
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Oxazoles
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Receptors, Mineralocorticoid
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oxazolidine