1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors

Bioorg Med Chem Lett. 2000 Jul 17;10(14):1555-8. doi: 10.1016/s0960-894x(00)00286-9.

Abstract

Structure-activity relationship within a series of 1-aminoalkylisoquinoline-4-carboxylates as inhibitors of DPP-IV is described. A primary aminomethyl group is required to maintain biological activity. Substitution of the isoquinoline at the 6- and 8-positions with methoxy groups increases potency to 53 times that of the lead compound SDZ 029-576.

MeSH terms

  • Carboxylic Acids / chemical synthesis*
  • Carboxylic Acids / chemistry
  • Carboxylic Acids / pharmacology
  • Colonic Neoplasms
  • Dipeptidyl Peptidase 4 / metabolism*
  • Humans
  • Indicators and Reagents
  • Isoquinolines / chemical synthesis*
  • Isoquinolines / chemistry
  • Isoquinolines / pharmacology
  • Kinetics
  • Molecular Structure
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Carboxylic Acids
  • Indicators and Reagents
  • Isoquinolines
  • Protease Inhibitors
  • Dipeptidyl Peptidase 4