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

Moiety Docking (animal) IC50
DOI: 10.1111/cbdd.13136 Publication Date: 2017-11-07T17:32:34Z
ABSTRACT
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.
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