Synthesis and acetylcholin esterase inhibition activity evaluation of some new hydroxyiminoindolin-2-one derivatives

Abstract

To create new drugs for Alzheimer as the most common form of dementia, based on the structural feature of the anti-alzheimer drug donepezil, 6 new hydroxyiminoindoline-2-one derivatives (4a-f) were prepared by  a 3-step synthetic pathway. The synthetic yield was moderate (c.a. 60 %). The AChE inhibition activity of the synthesized compounds was evaluated by Ellman method. All the 6 synthesized compounds were AchE-inhibitive. Especially, the 4f exhibited a significal activity (inhibited 51 % of donepezil’s activity on AChE). This proved the important role of methoxy group at position 5 and promise of a good activity of the derivatives by 6-methoxy group. and so, this proved in good accordanve to the researches by Sugimoto et al. in other series.