Literature DB >> 23777778

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

Christine Yang1, Hong C Shen, Zhicai Wu, Hong D Chu, Jason M Cox, Jaume Balsells, Alejandro Crespo, Patricia Brown, Beata Zamlynny, Judyann Wiltsie, Joseph Clemas, Jack Gibson, Lisa Contino, Jeanmarie Lisnock, Gaochao Zhou, Margarita Garcia-Calvo, Tom Bateman, Ling Xu, Xinchun Tong, Martin Crook, Peter Sinclair.   

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.

Entities:  

Mesh:

Substances:

Year:  2013        PMID: 23777778     DOI: 10.1016/j.bmcl.2013.05.077

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


  3 in total

Review 1.  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

2.  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

3.  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

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.