Design, Synthesis and Evaluation of Difunctionalized 4-Hydroxybenzaldehyde Derivatives as Novel Cholinesterase Inhibitors

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  • Yu Liang
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Cao Rihui
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Yi Wei
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Yan Qin
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Chen Zhiyong
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Ma Lin
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Song Huacan
    School of Chemistry and Chemical Engineering, Sun Yat-sen University

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A series of difunctionalized 4-hydroxybenzaldehyde derivatives were designed, synthesized and evaluated as cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)) inhibitors. The results demonstrated that all the compounds had more potent AChE and BChE inhibitory activities than galanthamine-HBr, one of the best cholinesterase inhibitors known so far. The inhibition mechanism revealed that the best active compound 4e displayed a mix-type mode of AChE and BChE by its dual-site interactions with the catalytic triad active center and the peripheral anionic site (PAS) of enzyme. All these data suggested that further development of such compounds may be of interest.

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