Design and synthesis of dual inhibitors of acetylcholinesterase and serotonin transporter targeting potential agents for Alzheimer's disease

Org Lett. 2002 Oct 3;4(20):3359-62. doi: 10.1021/ol026418e.

Abstract

Highly efficient acetylcholinesterase (AChE) and serotonin transporter (SERT) dual inhibitors, (S)-4 and (R)-13 were designed and synthesized on the basis of the hypothetical model of AChE active site. Both compounds showed potent inhibitory activities against AChE and SERT. [structure: see text]

MeSH terms

  • Acetylcholinesterase / chemistry
  • Acetylcholinesterase / metabolism
  • Alzheimer Disease / drug therapy*
  • Binding Sites
  • Cholinesterase Inhibitors / chemical synthesis*
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / metabolism
  • Cholinesterase Inhibitors / pharmacology
  • Drug Design*
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Selective Serotonin Reuptake Inhibitors / chemical synthesis*
  • Serotonin / metabolism

Substances

  • Cholinesterase Inhibitors
  • Serotonin Uptake Inhibitors
  • Serotonin
  • Acetylcholinesterase