Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: tetrahydrodiazabenzazulene derivatives

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1009-11. doi: 10.1016/s0960-894x(02)00090-2.

Abstract

Novel tetrahydrodiazabenzazulene derivatives, designed from the lead compound 1 discovered by screening of our in-house chemical library, were prepared and found to be potent neuropeptide Y-Y5 (NPY-Y5) receptor antagonists. The structure-activity relationships are described. Compounds 7 (FR240662) and 16 (FR252384) were especially attractive owing to their high affinities for the NPY-Y5 receptors, oral absorption and permeability to brain.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Azulenes
  • Benzoic Acid / chemistry
  • Binding Sites
  • Brain / drug effects
  • Brain / metabolism
  • Cycloheptanes / chemical synthesis*
  • Cycloheptanes / chemistry
  • Cycloheptanes / pharmacology*
  • Eating
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / pharmacology
  • Models, Molecular
  • Permeability / drug effects
  • Rats
  • Rats, Zucker
  • Receptors, Neuropeptide Y / antagonists & inhibitors*
  • Receptors, Neuropeptide Y / metabolism
  • Structure-Activity Relationship

Substances

  • Azulenes
  • Cycloheptanes
  • Heterocyclic Compounds
  • Receptors, Neuropeptide Y
  • neuropeptide Y5 receptor
  • azulene
  • Benzoic Acid