Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors

Bioorg Med Chem Lett. 2006 Jan 1;16(1):123-8. doi: 10.1016/j.bmcl.2005.09.037. Epub 2005 Oct 19.

Abstract

The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-(S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of dipeptidyl peptidase IV (DPP IV) are reported.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Binding Sites
  • Blood Glucose / metabolism
  • Caco-2 Cells
  • Chemistry, Pharmaceutical / methods*
  • Crystallography, X-Ray / methods*
  • Dipeptidyl Peptidase 4 / chemistry*
  • Dipeptidyl Peptidase 4 / metabolism
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Kinetics
  • Mice
  • Models, Chemical
  • Models, Molecular
  • Protease Inhibitors / pharmacology*
  • Rats
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Blood Glucose
  • Enzyme Inhibitors
  • Protease Inhibitors
  • Dipeptidyl Peptidase 4