Literature DB >> 24630411

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

Jason M Cox1, Hong D Chu2, Christine Yang2, Hong C Shen2, Zhicai Wu2, Jaume Balsells3, Alejandro Crespo4, Patricia Brown5, Beata Zamlynny5, Judyann Wiltsie6, Joseph Clemas6, Jack Gibson6, Lisa Contino6, JeanMarie Lisnock6, Gaochao Zhou6, Margarita Garcia-Calvo6, Thomas Bateman7, Ling Xu7, Xinchun Tong7, Martin Crook5, Peter Sinclair2.   

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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Hypertension; Lipophilic ligand efficiency; Mineralocorticoid receptor antagonist; Oxazolidinedione

Mesh：

Substances：

Year:  2014        PMID： 24630411     DOI： 10.1016/j.bmcl.2014.02.057

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Scaffold-hopping as a strategy to address metabolic liabilities of aromatic compounds.

Authors:  Phillip R Lazzara; Terry W Moore
Journal:  RSC Med Chem       Date:  2019-12-16

Review 2.  Third-generation Mineralocorticoid Receptor Antagonists: Why Do We Need a Fourth?

Authors:  Elise P Gomez-Sanchez
Journal:  J Cardiovasc Pharmacol       Date:  2016-01       Impact factor: 3.105

3.  Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.

Authors:  Christine Yang; Jaume Balsells; Hong D Chu; Jason M Cox; Alejandro Crespo; Xiuying Ma; Lisa Contino; Patricia Brown; Sheng Gao; Beata Zamlynny; Judyann Wiltsie; Joseph Clemas; JeanMarie Lisnock; Jack Gibson; Gaochao Zhou; Margarita Garcia-Calvo; Thomas J Bateman; Vincent Tong; Ling Xu; Martin Crook; Peter Sinclair; Hong C Shen
Journal:  ACS Med Chem Lett       Date:  2015-03-06       Impact factor: 4.345

Review 4.  Is there a new dawn for selective mineralocorticoid receptor antagonism?

Authors:  James M Luther
Journal:  Curr Opin Nephrol Hypertens       Date:  2014-09       Impact factor: 2.894

5.  Substrate-controlled selectivity switch in a three-component reaction: sequential synthesis of spiro-oxazolidinedione-cyclopentenones and hydroxy enaminobarbiturates in water.

Authors:  Mohammad Bagher Teimouri; Mahdi Heydari; Kazem Mohammadi
Journal:  RSC Adv       Date:  2020-04-03       Impact factor: 4.036
  5 in total

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