Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1739-42. doi: 10.1016/j.bmcl.2011.12.094. Epub 2011 Dec 28.

Abstract

Monoamine oxidase-B (MAO-B) inhibitor has been used as neuroprotectants to treat the motor deficits of Parkinson's disease (PD). We designed and synthesized a class of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors. The compounds have various inhibitory effects, with compound 6a having a K(i) value of 0.26 μM. Their promising activity in vitro suggests potential use in the treatment of PD.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry
  • Amides / pharmacology
  • Animals
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / chemistry
  • Benzimidazoles / pharmacology
  • Cell Line
  • Drug Design*
  • Enzyme Activation / drug effects
  • Humans
  • Mice
  • Molecular Structure
  • Monoamine Oxidase Inhibitors / chemical synthesis*
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Phenol / chemical synthesis
  • Phenol / chemistry
  • Phenol / pharmacology
  • Purines / chemical synthesis*
  • Purines / chemistry
  • Purines / pharmacology
  • Xanthines / chemical synthesis
  • Xanthines / chemistry
  • Xanthines / pharmacology

Substances

  • (E)-2-styryl-1-methylbenzimidazole
  • Amides
  • Benzimidazoles
  • Monoamine Oxidase Inhibitors
  • Purines
  • Xanthines
  • istradefylline
  • Phenol