Chemical Biology and Drug Design p. 756 - 762 (2018)
Update date:2022-09-26
Topics:
Wang, Jia
Wang, Chaolei
Wu, Zheng
Li, Xinnan
Xu, Shengtao
Liu, Jie
Lan, Qinying
Zhu, Zheying
Xu, Jinyi
A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory activities against AChE. Among them, compound 1q possessed the strongest anti-AChE activity with an IC50 value of 0.15?nm and high AChE/BuChE selectivity (SI?>?5,000). Moreover, compound 1q had low toxicity in normal nerve cells and was relatively stable in rat plasma. Together, the current finding may provide a new approach for the discovery of novel anti-Alzheimer's disease agents.
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