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目的改进土震素B类似物A环 2 烯 1 酮结构的合成路线 ,研究所合成的衍生物对新生大鼠原代培养海马神经元细胞缺糖缺氧损伤的保护作用。方法以 2 烯 伊比林酯为原料、溴代丁二酰亚胺代替三氧化铬为氧化剂合成目标化合物 ,溴代副产物经水解、氧化也转化为目标化合物。以大鼠原代培养海马神经元细胞缺糖缺氧损伤模型测试所合成化合物的活性。结果与结论共合成 4个未见文献报道的新化合物 ,经1H NMR和MS确证其结构。体外试验表明 :化合物 6b对大鼠原代培养海马神经元细胞缺糖缺氧损伤有较强的保护作用。
OBJECTIVE To improve the synthetic route of the 2-en-1 ketone structure of the A-ring analogues of tachykinin B, and to study the protective effect of the synthesized derivatives on the hypoxic-hypoxic injury of primary cultured hippocampal neurons in neonatal rats. Methods The target compounds were synthesized using 2-ene ibuprofen as raw material and bromosuccinimide instead of chromium trioxide as oxidant. The brominated by-products were hydrolyzed and converted to the target compounds. The activity of the synthesized compounds was tested in the rat primary cultured hippocampal neuronal cell model of hypoxia and hypoxia injury. RESULTS AND CONCLUSIONS Four new compounds were synthesized and their structures were confirmed by 1H NMR and MS. In vitro experiments showed that compound 6b had a strong protective effect on hypoxia and hypoxia injury in primary cultured rat hippocampal neurons.