The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I

Bioorg Med Chem Lett. 2000 Oct 2;10(19):2235-8. doi: 10.1016/s0960-894x(00)00449-2.

Abstract

This communication describes the synthesis and in vitro evaluation of a novel and potent series of phosphodiesterase type IV (PDE4) inhibitors. The compounds described represent conformationally constrained analogues of RP 73401, Piclamilast. Preliminary evidences of reduced side effects of II compared to standards are also reported.

MeSH terms

  • 3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
  • Benzamides / chemistry
  • Benzamides / pharmacology
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • Drug Design
  • Humans
  • Molecular Structure
  • Phosphodiesterase Inhibitors / chemical synthesis*
  • Phosphodiesterase Inhibitors / chemistry
  • Phosphodiesterase Inhibitors / pharmacology*
  • Phthalazines / chemical synthesis*
  • Phthalazines / chemistry
  • Phthalazines / pharmacology*
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Rolipram / chemistry
  • Rolipram / pharmacology

Substances

  • 1-(3,5-dichloropyrid-4-ylmethyl)-5-cyclopentoxy-6-methoxyphthalazine
  • Benzamides
  • Phosphodiesterase Inhibitors
  • Phthalazines
  • Pyridines
  • 3',5'-Cyclic-AMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • Rolipram
  • piclamilast