Phosphodiesterase 4 inhibitors as airways smooth muscle relaxant agents: synthesis and biological activities of triazine derivatives

Bioorg Med Chem. 1999 Mar;7(3):509-16. doi: 10.1016/s0968-0896(98)00266-1.

Abstract

A series of triazine derivatives was synthesized. The compounds were evaluated for tracheal smooth muscle relaxant and type 4 phosphodiesterase inhibitory activities. A highly significant correlation was observed between the two effects. Two compounds exhibited potent relaxant activity (EC50: 17 and 24 nM) and might be useful for the treatment of asthma.

MeSH terms

  • 3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
  • Animals
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • Guinea Pigs
  • In Vitro Techniques
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Molecular Structure
  • Muscle Relaxation / drug effects
  • Muscle, Smooth / drug effects*
  • Muscle, Smooth / physiology
  • Phosphodiesterase Inhibitors / pharmacology*
  • Rats
  • Trachea / drug effects*
  • Trachea / physiology
  • Triazines / chemical synthesis*
  • Triazines / chemistry
  • Triazines / pharmacology*

Substances

  • Phosphodiesterase Inhibitors
  • Triazines
  • 3',5'-Cyclic-AMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 4