2000 Vol.11 No.8 P.Preparation of AChE Inhibitors From Jujubogenin

A dammarane derivative dihydrojujubogenin-2-en-1-one, which possesses a skeleton and pharmacophore partially similar to those of Territrem B, a potent AChE inhibitor, was synthesized via three different paths. The anti-AChE activity of this compound and related analogue was measured.     

Preparation of AChE Inhibitors From Jujubogenin

The advanced medical technology has lengthened the life expectancy of human beings.This makes some previously ignored diseases prominent, such as Alzheimer disease(AD). The low level of acetylcholine (ACh) in brain is considered to be one of mainreasons for suffering such memory loss disease. Thereby, how to elevate ACh level inbrain and enhance the cognition has become a main issue l'2. One of the approaches is toinvestigate acetylcholinesterase (AChE) inhibitors, which can prevent the hy…     

Synthesis of 2-En-1-one-ebelactonyl Benzoates of Territrem B Analogues from Jujubogenin

AChE inhibitors are important target on drug discovery for the treatment of Alzheimerdisease. Tacrine 1, E2020 2 as well as huperzine A 3 are the few distinguishedsuccessful leading compounds in this aspect1 . ～3 Recently, the potential activity ofterritrem B (Figure 1) on AChE inhibition (IC50 =7.8 nmol/L) led to a wide interest.Furthermore, its inhibitory mechanism is totally different from the known AChEinhibitors3 . The interest in synthesis of new leading compounds was l…