[Design, synthesis and in vitro activity of glycinamide-bearing compounds as DPP-IV inhibitors]

Yao Xue Xue Bao. 2010 Nov;45(11):1379-84.
[Article in Chinese]

Abstract

To research the structure-activity relationship (SAR) of glycinamide-bearing compounds that used as inhibitors of dipeptidyl peptidase IV (DPP-IV), P32/98 and compound A were chosen as the leading compounds, heterocycles containing nitrogen atom were introduced to form amide, and different residues on a-position of carbonyl were designed. The nineteen designed compounds were synthesized by a simple route and were evaluated as inhibitors of DPP-IV. All of the structures were characterized by 1H NMR and HRMS. The preliminary SAR result was obtained.

Publication types

  • English Abstract
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Dipeptidyl Peptidase 4 / metabolism*
  • Dipeptidyl-Peptidase IV Inhibitors / chemical synthesis*
  • Dipeptidyl-Peptidase IV Inhibitors / chemistry
  • Dipeptidyl-Peptidase IV Inhibitors / pharmacology
  • Drug Design
  • Glycine / analogs & derivatives*
  • Glycine / chemistry
  • Magnetic Resonance Spectroscopy / methods
  • Molecular Structure
  • Piperazines / chemistry
  • Piperazines / pharmacology
  • Structure-Activity Relationship

Substances

  • Dipeptidyl-Peptidase IV Inhibitors
  • Piperazines
  • glycine amide
  • 1-ethyl-2,3-dioxopiperazine
  • Dipeptidyl Peptidase 4
  • Glycine