土震素B类似物中A环2-烯-1-酮结构的合成方法改进及衍生物抗脑缺血活性Improved synthesis of 2-en-1-one moiety in the Aring of territrem B analogues and evaluation of their protective effect against brain ischemia injury
赵金浩,赵锋,李海波,巫秀美,王彦广,蒋华良,赵昱
摘要(Abstract)：
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。
关键词(KeyWords)： 药物化学;制备;化学合成;土震素B类似物;2烯1酮结构;抗缺糖缺氧损伤
基金项目(Foundation):
作者(Author): 赵金浩,赵锋,李海波,巫秀美,王彦广,蒋华良,赵昱
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