Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors

Bioorg Med Chem Lett. 2002 Mar 25;12(6):865-8. doi: 10.1016/s0960-894x(02)00030-6.

Abstract

2-aryl-substituted imidazo[5,1-f][1,2,4]triazin-4(3H)-ones represent a new class of potent cGMP-PDE 5 inhibitors that prove to be superior to other purine-isosteric inhibitors. Subnanomolar inhibitors of PDE 5 with activity in in vivo models for erectile dysfunction have been identified. BAY 38-9456 (Vardenafil-hydrochloride) has been selected for clinical studies in the indication of erectile dysfunction.

MeSH terms

  • 3',5'-Cyclic-GMP Phosphodiesterases / antagonists & inhibitors*
  • 3',5'-Cyclic-GMP Phosphodiesterases / metabolism
  • Animals
  • Cyclic Nucleotide Phosphodiesterases, Type 5
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Erectile Dysfunction / drug therapy
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology
  • Inhibitory Concentration 50
  • Male
  • Protein Binding
  • Rabbits
  • Structure-Activity Relationship
  • Triazines / chemical synthesis
  • Triazines / pharmacology

Substances

  • Enzyme Inhibitors
  • Imidazoles
  • Triazines
  • 3',5'-Cyclic-GMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 5