(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: Bell MG; Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. bell_michael_g@Lilly.com, Gernert DL, Grese TA, Belvo MD, Borromeo PS, Kelley SA, Kennedy JH, Kolis SP, Lander PA, Richey R, Sharp VS, Stephenson GA, Williams JD, Yu H, Zimmerman KM, Steinberg MI, Jadhav PK
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2007 Dec 27; Vol. 50 (26), pp. 6443-5. Date of Electronic Publication: 2007 Nov 27.
DOI: 10.1021/jm701186z
Abstrakt: 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: MEDLINE