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.
MeSH terms
-
Animals
-
Antihypertensive Agents / chemical synthesis*
-
Antihypertensive Agents / chemistry
-
Antihypertensive Agents / pharmacology
-
Crystallography, X-Ray
-
Indoles / chemical synthesis*
-
Indoles / chemistry
-
Indoles / pharmacology
-
Mineralocorticoid Receptor Antagonists*
-
Models, Molecular
-
Rats
-
Rats, Sprague-Dawley
-
Stereoisomerism
-
Structure-Activity Relationship
-
Sulfonamides / chemical synthesis*
-
Sulfonamides / chemistry
-
Sulfonamides / pharmacology
Substances
-
Antihypertensive Agents
-
Indoles
-
Mineralocorticoid Receptor Antagonists
-
N-(3-(1-cyclopropyl-1-(2,4-difluorophenyl)ethyl)-1H-indol-7-yl)methanesulfonamide
-
Sulfonamides