Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1337-40. doi: 10.1016/j.bmcl.2005.01.020.

Abstract

A new series of pyrazolidine derivatives was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 9i was the most active in this series, exhibited IC50 value of 1.56 microM and ED50 value of 80 mg/kg (in vivo DP-IV inhibition; po).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Dipeptidyl Peptidase 4 / drug effects*
  • Enzyme Inhibitors* / chemical synthesis
  • Enzyme Inhibitors* / pharmacology
  • Molecular Structure
  • Pyrazoles* / chemical synthesis
  • Pyrazoles* / pharmacology
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Pyrazoles
  • Dipeptidyl Peptidase 4