Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors

Bioorg Med Chem Lett. 2001 Mar 12;11(5):611-4. doi: 10.1016/s0960-894x(00)00681-8.

Abstract

The syntheses and in vitro evaluation of a new series of pyrido[2,3-d]pyrimidine-2,4-diones bearing substituents at C-3 and/or C-4 positions on the pyridine ring are described. Some of these compounds, especially 51 and 6f, were found to be potent phosphodiesterase 4 (PDE 4) inhibitors exhibiting improved ratio of PDE 4 inhibitory activity:rolipram binding assay (RBA).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
  • 3',5'-Cyclic-AMP Phosphodiesterases / metabolism
  • Animals
  • Biological Assay
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • Humans
  • Molecular Structure
  • Phosphodiesterase Inhibitors / chemical synthesis*
  • Phosphodiesterase Inhibitors / chemistry
  • Phosphodiesterase Inhibitors / pharmacology*
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / metabolism
  • Pyrimidines / pharmacology*
  • Quinazolines / chemical synthesis*
  • Quinazolines / chemistry*
  • Quinazolines / pharmacology*
  • Rats
  • Rolipram / metabolism

Substances

  • CP 77059
  • Phosphodiesterase Inhibitors
  • Pyrimidines
  • Quinazolines
  • RS 25344
  • 3',5'-Cyclic-AMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • Rolipram