Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors

Bioorg Med Chem Lett. 1999 Aug 16;9(16):2335-8. doi: 10.1016/s0960-894x(99)00396-0.

Abstract

Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperzine A and an intact tacrine unit were prepared. The syntheses are quite direct, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (+/-)-9g is 13-fold more potent than (-)-huperzine A, and 25-fold more potent than tacrine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / drug effects*
  • Alkaloids
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / pharmacology*
  • Sesquiterpenes / chemistry*
  • Tacrine / chemistry*

Substances

  • Alkaloids
  • Cholinesterase Inhibitors
  • Sesquiterpenes
  • huperzine A
  • Tacrine
  • Acetylcholinesterase