Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors

Bioorg Med Chem Lett. 2003 Jun 16;13(12):1981-4. doi: 10.1016/s0960-894x(03)00351-2.

Abstract

Dihydroquinolines with aminoalkyl side chains have been synthesized and have been shown to be potent n-NOS inhibitors. A marked selectivity versus e-NOS of up to approximately 300-fold was observed, whereas i-NOS was moderately inhibited.

MeSH terms

  • Amines / chemistry*
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Nitric Oxide Synthase / antagonists & inhibitors*
  • Nitric Oxide Synthase Type I
  • Nitric Oxide Synthase Type II
  • Nitric Oxide Synthase Type III
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Recombinant Proteins / antagonists & inhibitors
  • Reference Values
  • Structure-Activity Relationship

Substances

  • Amines
  • Enzyme Inhibitors
  • Quinolines
  • Recombinant Proteins
  • NOS1 protein, human
  • NOS2 protein, human
  • NOS3 protein, human
  • Nitric Oxide Synthase
  • Nitric Oxide Synthase Type I
  • Nitric Oxide Synthase Type II
  • Nitric Oxide Synthase Type III