Articles

Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.

Author

Carlier PR, Du DM, Han Y, Liu J

Date

16/8/1999

Journal

Bioorg Med Chem Lett

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.