Potent and selective proline derived dipeptidyl peptidase IV inhibitors

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5151-5. doi: 10.1016/j.bmcl.2004.07.056.

Abstract

In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50=1.9 microM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Dipeptidyl Peptidase 4 / metabolism*
  • Humans
  • In Vitro Techniques
  • Proline / analogs & derivatives*
  • Proline / chemical synthesis*
  • Proline / chemistry
  • Proline / pharmacology
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology
  • Rats
  • Structure-Activity Relationship

Substances

  • Protease Inhibitors
  • Proline
  • Dipeptidyl Peptidase 4