Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3900-7. doi: 10.1016/j.bmcl.2005.05.090.

Abstract

Several different heterocyclic systems were compared as PDE5 inhibitor scaffolds. In addition to the known 3H-imidazo[5,1-f][1,2,4]triazin-4-ones and pyrazolopyrimidinones, isomeric imidazo[1,5-a][1,3,5]triazin-4(3H)-ones were also shown to be potent and selective PDE inhibitor scaffolds with in vivo activity. SAR trends were elucidated for sulfonamide derivatives with generality across different scaffolds.

Publication types

  • Comparative Study

MeSH terms

  • 3',5'-Cyclic-GMP Phosphodiesterases / antagonists & inhibitors*
  • Cyclic Nucleotide Phosphodiesterases, Type 5
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / pharmacology
  • Inhibitory Concentration 50
  • Structure-Activity Relationship
  • Substrate Specificity

Substances

  • Heterocyclic Compounds
  • 3',5'-Cyclic-GMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 5