New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors

Bioorg Med Chem Lett. 2005 May 2;15(9):2381-4. doi: 10.1016/j.bmcl.2005.02.090.

Abstract

A series of potent PDE5 inhibitors with high selectivity versus PDE6 isoenzymes was identified.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3',5'-Cyclic-GMP Phosphodiesterases
  • Animals
  • Blood Platelets / enzymology
  • Cattle
  • Cyclic Nucleotide Phosphodiesterases, Type 5
  • Cyclic Nucleotide Phosphodiesterases, Type 6
  • Molecular Structure
  • Phosphodiesterase Inhibitors / chemical synthesis*
  • Phosphodiesterase Inhibitors / pharmacology*
  • Phosphoric Diester Hydrolases / blood
  • Phosphoric Diester Hydrolases / metabolism*
  • Pyrazoles / chemical synthesis
  • Pyrazoles / pharmacology
  • Pyridazines / chemical synthesis*
  • Pyridazines / pharmacology*
  • Retina / enzymology
  • Sensitivity and Specificity
  • Structure-Activity Relationship

Substances

  • Phosphodiesterase Inhibitors
  • Pyrazoles
  • Pyridazines
  • Phosphoric Diester Hydrolases
  • 3',5'-Cyclic-GMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 5
  • Cyclic Nucleotide Phosphodiesterases, Type 6