Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists.
The characterization of a novel series of NPY-1 receptor antagonists derived from the 4-methylbenzimidazole 4 is described. Appropriate substitution on the piperidyl nitrogen of 4 led to systematic increases in Y-1 receptor affinity, to approximately 50-fold, and to the discovery of the importance of a second basic substituent.
Zimmerman
D M
DM
Eli Lilly and Company, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Cantrell
B E
BE
Smith
E C
EC
Nixon
J A
JA
Bruns
R F
RF
Gitter
B
B
Hipskind
P A
PA
Ornstein
P L
PL
Zarrinmayeh
H
H
Britton
T C
TC
Schober
D A
DA
Gehlert
D R
DR
D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D017476:Receptors, Neuropeptide Y; D011994:Recombinant Proteins