title: Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists.
abstract: 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.
authors.affiliation: Eli Lilly and Company, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA.
authors.forename: D M
authors.initials: DM
authors.lastname: Zimmerman
authors.forename: B E
authors.initials: BE
authors.lastname: Cantrell
authors.forename: E C
authors.initials: EC
authors.lastname: Smith
authors.forename: J A
authors.initials: JA
authors.lastname: Nixon
authors.forename: R F
authors.initials: RF
authors.lastname: Bruns
authors.forename: B
authors.initials: B
authors.lastname: Gitter
authors.forename: P A
authors.initials: PA
authors.lastname: Hipskind
authors.forename: P L
authors.initials: PL
authors.lastname: Ornstein
authors.forename: H
authors.initials: H
authors.lastname: Zarrinmayeh
authors.forename: T C
authors.initials: TC
authors.lastname: Britton
authors.forename: D A
authors.initials: DA
authors.lastname: Schober
authors.forename: D R
authors.initials: DR
authors.lastname: Gehlert
mesh_terms: 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
chemical_list: D001562:Benzimidazoles; D017476:Receptors, Neuropeptide Y; D011994:Recombinant Proteins