Synthesis of 9-Aminoacridine Derivatives as Anti-Alzheimer Agents

Am J Alzheimers Dis Other Demen. 2016 May;31(3):263-9. doi: 10.1177/1533317515603115. Epub 2015 Sep 17.

Abstract

In the present study, some 9-aminoacridine derivatives have been synthesized by condensation of 9-aminoacridine with substituted phenacyl, benzoyl, and benzyl halides (RM1-RM6). Compounds were investigated for acetylcholinesterase and butyrylcholinesterase inhibition potential, considering these enzymes playing a key role in Alzheimer's disease. All derivatives showed better inhibition of enzymes than the standard galantamine, whereas except RM4, all exhibit better results than tacrine, a well-known acridine derivative used for the treatment of Alzheimer's disease.

Keywords: 9-aminoacridine (9AA); Alzheimer; acetylcholinesterase (AChE); butyrylcholinesterase (BuChE); cholinesterases (ChE); tacrine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alzheimer Disease / drug therapy
  • Alzheimer Disease / enzymology*
  • Aminacrine / chemical synthesis*
  • Cholinesterase Inhibitors / chemical synthesis*
  • Humans
  • In Vitro Techniques

Substances

  • Cholinesterase Inhibitors
  • Aminacrine