Nicotinamide ethers: novel inhibitors of calcium-independent phosphodiesterase and [3H]rolipram binding

J Med Chem. 1991 Jan;34(1):86-9. doi: 10.1021/jm00105a015.

Abstract

The synthesis and biological properties of a series of nicotinamide ethers are described. These compounds, structurally novel calcium-independent phosphodiesterase inhibitors, also inhibit the binding of [3H]rolipram to rat brain membranes and reverse reserpine-induced hypothermia in the mouse. Several compounds exhibited potent in vivo activity comparable to the standard agent, rolipram.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Binding Sites
  • Body Temperature Regulation / drug effects
  • Brain / metabolism*
  • Ethers
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Mice
  • Molecular Structure
  • Niacinamide / analogs & derivatives*
  • Niacinamide / chemical synthesis*
  • Niacinamide / pharmacology
  • Phosphodiesterase Inhibitors / chemical synthesis*
  • Protein Binding
  • Pyrrolidinones / metabolism*
  • Pyrrolidinones / pharmacology
  • Rats
  • Reserpine / pharmacology
  • Rolipram
  • Structure-Activity Relationship

Substances

  • Ethers
  • Indicators and Reagents
  • Phosphodiesterase Inhibitors
  • Pyrrolidinones
  • Niacinamide
  • Reserpine
  • Rolipram