(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.
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.
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. bell_michael_g@Lilly.com
Michael G
MG
Bell
Douglas L
DL
Gernert
Timothy A
TA
Grese
Matthew D
MD
Belvo
Peter S
PS
Borromeo
Sally A
SA
Kelley
Joseph H
JH
Kennedy
Stanley P
SP
Kolis
Peter A
PA
Lander
Rachel
R
Richey
V Scott
VS
Sharp
Gregory A
GA
Stephenson
Jeffrey D
JD
Williams
Hannah
H
Yu
Karen M
KM
Zimmerman
Mitchell I
MI
Steinberg
Prabhakar K
PK
Jadhav
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000451:Mineralocorticoid Receptor Antagonists; D008958:Models, Molecular; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000959:Antihypertensive Agents; D007211:Indoles; D000451:Mineralocorticoid Receptor Antagonists; C527716:N-(3-(1-cyclopropyl-1-(2,4-difluorophenyl)ethyl)-1H-indol-7-yl)methanesulfonamide; D013449:Sulfonamides