Longanlactone analogues were synthesized using a route featuring Friedel-Crafts acylation, Sonogashira coupling and 1,3-dipolar cycloaddition reactions. Structure–activity relationships were investigated for neurotrophic activity. Compound 6 was found to have the most potent neurotrophic activity among all the synthesized analogues in Neuro2a cells as evidenced by a battery of in vitro/cell based assays for assessment of neurogenic and potential neurotrophic activity including neurite outgrowth assay and real time PCR for popular markers of augmented neurotrophic activity. Compound 6 might serve as a template for further development of highly effective neurotrophic molecules.

使用以Friedel-Crafts酰化，Sonogashira偶联和1,3-偶极环加成反应为特征的途径合成Longanlactone类似物。研究了结构-活动关系的神经营养活动。发现化合物6在Neuro2a细胞中所有合成的类似物中具有最强的神经营养活性，这一点已通过一系列基于神经/潜在神经营养活性的体外/细胞试验（包括神经突增生试验和实时PCR进行流行的标记物评估）得到证明。增强的神经营养活动。化合物6可以用作进一步开发高效神经营养分子的模板。