Synthesis and SAR Studies of Neuritogenic Gentiside Derivatives

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  • Wang Guangfa
    College of Pharmaceutical Sciences, Zhejiang University
  • Bian Linglin
    College of Pharmaceutical Sciences, Zhejiang University
  • Zhang Hui
    College of Pharmaceutical Sciences, Zhejiang University
  • Wang Yanhui
    College of Pharmaceutical Sciences, Zhejiang University
  • Gao Lijuan
    College of Pharmaceutical Sciences, Zhejiang University
  • Sun Kaiyue
    College of Pharmaceutical Sciences, Zhejiang University
  • Xiang Lan
    College of Pharmaceutical Sciences, Zhejiang University
  • Qi Jianhua
    College of Pharmaceutical Sciences, Zhejiang University

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Tetradecyl 2,3-dihydroxybenzoate (ABG-001) has been designed and synthesised as a lead compound to treat Alzheimer’s disease, based on structure–activity relationships of gentisides. In this paper, the alkyl chain and ester linkage group of ABG-001 were modified. Consequently, several series of novel gentiside derivatives were designed and synthesised, and their neuritogenic activity was evaluated in PC12 cells. Among all the tested compounds, S-dodecyl 2,3-dihydroxybenzothioate (15d, named as ABG-199) was the most potent; the compound induced significant neurite outgrowth at 0.1 µM, which was comparable to that of nerve growth factor at the optimal concentration of 40 ng/mL and ABG-001 at 1 µM. A brief study on the mechanism of action of ABG-199 revealed that extracellular signal-regulated kinase phosphorylation was involved in ABG-199-induced neurite outgrowth in PC12 cells.

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