Literature DB >> 18038968

(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.

Michael G Bell1, Douglas L Gernert, Timothy A Grese, Matthew D Belvo, Peter S Borromeo, Sally A Kelley, Joseph H Kennedy, Stanley P Kolis, Peter A Lander, Rachel Richey, V Scott Sharp, Gregory A Stephenson, Jeffrey D Williams, Hannah Yu, Karen M Zimmerman, Mitchell I Steinberg, Prabhakar K Jadhav.   

Abstract

A novel, potent series of indole analogs were recently developed as MR antagonists, culminating in 14. This compound represents the first MR antagonist in this class of molecules, exhibiting picomolar binding affinity and in vivo blood pressure lowering at pharmaceutically relevant doses.

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Year:  2007        PMID: 18038968     DOI: 10.1021/jm701186z

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  6 in total

1.  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

2.  Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.

Authors:  Timothy I Richardson; Christian A Clarke; Kuo-Long Yu; Ying K Yee; Thomas J Bleisch; Jose E Lopez; Scott A Jones; Norman E Hughes; Brian S Muehl; Charles W Lugar; Terry L Moore; Pamela K Shetler; Richard W Zink; John J Osborne; Chahrzad Montrose-Rafizadeh; Nita Patel; Andrew G Geiser; Rachelle J Sells Galvin; Jeffrey A Dodge
Journal:  ACS Med Chem Lett       Date:  2010-12-09       Impact factor: 4.345

3.  The mineralocorticoid receptor antagonist spironolactone reduces alcohol self-administration in female and male rats.

Authors:  Viren H Makhijani; Kalynn Van Voorhies; Joyce Besheer
Journal:  Pharmacol Biochem Behav       Date:  2018-08-29       Impact factor: 3.533

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.  Palladium-Catalyzed Atom-Transfer Radical Cyclization at Remote Unactivated C(sp3 )-H Sites: Hydrogen-Atom Transfer of Hybrid Vinyl Palladium Radical Intermediates.

Authors:  Maxim Ratushnyy; Marvin Parasram; Yang Wang; Vladimir Gevorgyan
Journal:  Angew Chem Int Ed Engl       Date:  2018-02-06       Impact factor: 15.336

6.  Rh(iii)-catalyzed C-7 arylation of indolines with arylsilanes via C-H activation.

Authors:  Haiqing Luo; Qi Xie; Kai Sun; Jianbo Deng; Lin Xu; Kejun Wang; Xuzhong Luo
Journal:  RSC Adv       Date:  2019-06-10       Impact factor: 4.036

  6 in total

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