The design and synthesis of novel inhibitors of NADH:ubiquinone oxidoreductase

Bioorg Med Chem Lett. 2004 Jan 19;14(2):511-4. doi: 10.1016/j.bmcl.2003.10.022.

Abstract

Potent new inhibitors of NADH:ubiquinone oxidoreductase (complex I) have been designed, with the help of molecular modelling, by hybridisation of known complex I inhibitors with inhibitors of cytochrome c oxidoreductase. The most interesting compound was the chromone 7 which was a selective inhibitor of complex I (IC(50) 15 nM) and showed acaricidal activity against spider mites.

MeSH terms

  • Animals
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Electron Transport Complex I / antagonists & inhibitors*
  • Electron Transport Complex I / metabolism
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Houseflies
  • Phaseolus / parasitology
  • Tetranychidae

Substances

  • Enzyme Inhibitors
  • Electron Transport Complex I