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.


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


  • Benzimidazoles
  • Receptors, Neuropeptide Y
  • Recombinant Proteins