(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

Autor:	Matthew D. Belvo, Michael Gregory Bell, Douglas Linn Gernert, V. Scott Sharp, Joseph H. Kennedy, Hannah Yu, Peter Stanley Borromeo, Timothy Alan Grese, Sally Ann Kelley, Gregory A. Stephenson, Mitchell I. Steinberg, Prabhakar Kondaji Jadhav, Jeffrey D. Williams, Karen M. Zimmerman, Rachel N. Richey, Stanley P. Kolis, Peter Ambrose Lander
Rok vydání:	2007
Předmět:	Models Molecular Indole test Sulfonamides Indoles Stereochemistry Chemistry Antagonist Stereoisomerism Biological activity Crystallography X-Ray Chemical synthesis Rats Rats Sprague-Dawley Structure-Activity Relationship Mineralocorticoid receptor In vivo Drug Discovery Animals Molecular Medicine Structure–activity relationship Antihypertensive Agents Mineralocorticoid Receptor Antagonists
Zdroj:	Journal of Medicinal Chemistry. 50:6443-6445
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm701186z
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d7278bc07b6e6e72013351da2997c964 https://doi.org/10.1021/jm701186z Zobrazit plný text záznamu