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
基于
龙胆苷的结构-活性关系,设计并合成了
2,3-二羟基苯甲酸十四烷基酯(ABG-001)作为治疗阿尔茨海默氏病的先导化合物。本文对ABG-001的烷基链和酯键进行了修饰。因此,设计和合成了一系列新的
龙胆苷衍
生物,并在PC12细胞中评估了它们的神经生成活性。在所有测试的化合物中,S-
十二烷基2,3-二羟基苯甲
硫醇酯(15d,命名为ABG-199)是最有效的。该化合物在0.1 microM时诱导明显的神经突长出,与最佳浓度40 ng / mL的神经生长因子和1 microM的ABG-001相当。