Design, synthesis, biological evaluation, and docking study of 4‐isochromanone hybrids bearing N‐benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II)

• DOI: 10.1111/cbdd.13136
• Publication Date: 2017-11-07T17:32:34Z
• Authors: Jia Wang; Chaolei Wang; Zheng Wu; Xinnan Li; Shengtao Xu; Jie Liu; Qinying Lan; Zheying Zhu; Jinyi Xu
• Keywords: Moiety; Docking (animal); IC50

A series of novel 4‐isochromanone compounds bearing N ‐benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase ( AC hE) inhibitors. The biological evaluation showed that most the target exhibited potent inhibitory activities against hE. Among them, compound 1q possessed strongest anti‐ hE activity with an IC 50 value 0.15 n m high hE/BuChE selectivity SI > 5,000). Moreover, had low toxicity in normal nerve cells was relatively stable rat plasma. Together, current finding may provide a new approach for discovery anti‐Alzheimer's disease agents.