Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors

Bioorganic & Medicinal Chemistry Letters
1999.0

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.

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