Structure-Activity studies for a novel series of tricyclic dihydropyrimidines as K(ATP) channel openers (KCOs)

Bioorg Med Chem Lett. 2002 Jun 3;12(11):1481-4. doi: 10.1016/s0960-894x(02)00207-x.

Abstract

A novel series of tricyclic dihydropyrimidines was synthesized and evaluated for activity as K(ATP) channel openers. The functional activity of several compounds, for example 6A (EC(50)=30nM) and its enantiomers exceeded cromakalim.

MeSH terms

  • Animals
  • Cell Culture Techniques
  • Cromakalim / pharmacology
  • Fluorescence
  • Guanidines / administration & dosage
  • Guanidines / pharmacokinetics
  • Guinea Pigs
  • Heterocyclic Compounds, 3-Ring / chemical synthesis*
  • Heterocyclic Compounds, 3-Ring / chemistry
  • Heterocyclic Compounds, 3-Ring / pharmacokinetics
  • Heterocyclic Compounds, 3-Ring / pharmacology*
  • Membrane Potentials / drug effects
  • Potassium Channels / agonists
  • Potassium Channels / drug effects*
  • Pyridines / administration & dosage
  • Pyridines / pharmacokinetics
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacokinetics
  • Pyrimidines / pharmacology*
  • Structure-Activity Relationship
  • Urinary Bladder / chemistry
  • Urinary Bladder / drug effects

Substances

  • Guanidines
  • Heterocyclic Compounds, 3-Ring
  • Potassium Channels
  • Pyridines
  • Pyrimidines
  • Cromakalim
  • N-cyano-N'-(1,1-dimethylpropyl)-N''-(3-pyridinyl)guanidine