Synthesis of (±)-10,10-dimethylhuperzine A — a huperzine analogue possessing a slower enzyme off-rate

Bioorganic & Medicinal Chemistry Letters
1996.0

Abstract

The synthesis of (+)-10,10-dimethylhuperzine A is reported together with its kinetic (k_on and k_off) and dissociation constants for the inhibition of fetal bovine serum acetylcholinesterase. While somewhat more potent than (±)-huperzine A, the dimethyl analogue shows a slower off-rate from AChE, a result that may be of potential therapeutic value.

DOI： 10.1016/0960-894X(96)00012-1

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