Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists

D M Zimmerman; B E Cantrell; E C Smith; J A Nixon; R F Bruns; B Gitter; P A Hipskind; P L Ornstein; H Zarrinmayeh; T C Britton; D A Schober; D R Gehlert

doi:10.1016/s0960-894x(98)00048-1

Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists

Bioorg Med Chem Lett. 1998 Mar 3;8(5):473-6. doi: 10.1016/s0960-894x(98)00048-1.

Authors

D M Zimmerman¹, B E Cantrell, E C Smith, J A Nixon, R F Bruns, B Gitter, P A Hipskind, P L Ornstein, H Zarrinmayeh, T C Britton, D A Schober, D R Gehlert

Affiliation

¹ Eli Lilly and Company, Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA.

PMID: 9871601
DOI: 10.1016/s0960-894x(98)00048-1

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.

MeSH terms

Benzimidazoles / chemistry*
Benzimidazoles / pharmacology*
Cell Line
Receptors, Neuropeptide Y / antagonists & inhibitors*
Recombinant Proteins / antagonists & inhibitors
Structure-Activity Relationship

Substances

Benzimidazoles
Receptors, Neuropeptide Y
Recombinant Proteins