Synthesis and acetylcholinesterase inhibitory activity of several pyrimidone analogues of huperzine A
Abstract
Syntheses of four new pyrimidone analogues of the acetylcholinesterase (AChE) inhibitor huperzine A are reported together with the inhibitory potencies of these compounds for foetal bovine calf serum AChE; β-lactone formation followed by a thermal cycloreversion reaction serves as the key step for introduction of the ethylidene appendage of 12 in the stereochemically correct form.