Synthesis and biological evaluation of 2,5-dihydropyrazol

Bioorg Med Chem Lett. 2000 Dec 4;10(23):2661-4. doi: 10.1016/s0960-894x(00)00548-5.

Abstract

A novel series of 2,5-dihydropyrazolo[4,3-c]quinolin-3-ones has been prepared. These compounds showed good PDE 4 inhibitory activity and weak affinity for rolipram's binding site. They also exhibited a good anti-inflammatory profile without emetic side effects.

MeSH terms

  • Animals
  • Anti-Asthmatic Agents / chemical synthesis
  • Anti-Asthmatic Agents / chemistry
  • Anti-Asthmatic Agents / pharmacology
  • Emetics / chemical synthesis
  • Emetics / chemistry
  • Emetics / pharmacology
  • Guinea Pigs
  • In Vitro Techniques
  • Models, Molecular
  • Phosphodiesterase Inhibitors / chemical synthesis*
  • Phosphodiesterase Inhibitors / chemistry
  • Phosphodiesterase Inhibitors / pharmacology
  • Quinolones / chemical synthesis*
  • Quinolones / chemistry
  • Quinolones / pharmacology*
  • Structure-Activity Relationship

Substances

  • Anti-Asthmatic Agents
  • Emetics
  • Phosphodiesterase Inhibitors
  • Quinolones