Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors

Bioorg Med Chem Lett. 1999 Jan 4;9(1):7-12. doi: 10.1016/s0960-894x(98)00681-7.

Abstract

Syntheses and structure-activity relationships (SAR) of cGMP selective phosphodiesterase inhibitors are discussed. Potent and selective inhibitors are produced when the C-2 position of tetracyclic guanine 1 is substituted with alkyl chains containing six carbon atoms.

MeSH terms

  • 3',5'-Cyclic-GMP Phosphodiesterases / antagonists & inhibitors*
  • Drug Evaluation, Preclinical
  • Guanine / chemistry
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry*
  • Imidazoles / pharmacology*
  • Inhibitory Concentration 50
  • Isoenzymes
  • Phosphodiesterase Inhibitors / chemical synthesis
  • Phosphodiesterase Inhibitors / chemistry*
  • Phosphodiesterase Inhibitors / pharmacology*
  • Purines / chemical synthesis
  • Purines / chemistry*
  • Purines / pharmacology*
  • Structure-Activity Relationship

Substances

  • 1,2,6,8b-tetrahydro-5-methyl-2-(1-methylethyl)-7-(4-methylpentyl)imidazo(2,1-e)purine-5(4H)-one
  • Imidazoles
  • Isoenzymes
  • Phosphodiesterase Inhibitors
  • Purines
  • Guanine
  • 3',5'-Cyclic-GMP Phosphodiesterases