Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists

Bioorg Med Chem Lett. 2000 Jun 5;10(11):1175-9. doi: 10.1016/s0960-894x(00)00177-3.


The design of a novel series of NPY-Y5 receptor antagonists is described. Key elements for the design were the identification of weak Y5 hits from a Y1 program, results from a combinatorial approach and database mining. This led to the discovery of the quinazoline 4 and the aryl-sulphonamide moiety as major components of the pharmacophore for Y5 affinity. The synthesis and SAR towards CGP71683A is described.

MeSH terms

  • Drug Design
  • Models, Molecular
  • Quinazolines / chemical synthesis*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology
  • Receptors, Neuropeptide Y / antagonists & inhibitors*
  • Structure-Activity Relationship


  • Quinazolines
  • Receptors, Neuropeptide Y
  • neuropeptide Y5 receptor