A new series of ligustrazine-cinnamon acid derivatives had been designed and synthesized as potential neuro-protective agents. Among the derivatives, 3a exhibited the promising neuroprotective activity (EC₅₀ = 3.68 μM). Moreover, with the deep research of the drug pathway, it (the further mechanism researches) suggested compound 3a could inhibit the apoptosis of injured PC12 cells via blocking the mitochondria apoptosis pathway including up-regulation the ratio of Bcl-2/Bax, down-regulation the expression of cytochrome-c (Cyt-c) and inhibition of the activity of caspase-9 and -3. In addition, the structure-activity relationships (SARs) of novel compounds were also discussed.

已经设计并合成了一系列新的川gust嗪肉桂酸衍生物作为潜在的神经保护剂。在衍生物中，3a表现出有希望的神经保护活性（EC ₅₀  = 3.68μM）。此外，随着对药物途径的深入研究，它（进一步的机理研究）表明化合物3a可以通过阻断线粒体凋亡途径（包括上调Bcl-2 / Bax的比例，降低细胞凋亡率）来抑制受损的PC12细胞的凋亡。调节细胞色素c（Cyt c）的表达并抑制caspase-9和-3的活性。此外，还讨论了新型化合物的构效关系（SAR）。