摘要
目的合成新型吡咯烷类神经氨酸酶抑制剂,并测定其抑制神经氨酸酶的活性。方法以L-羟脯氨酸为原料,合成一系列神经氨酸酶抑制剂,并用高通量活性筛选方法检测其对神经氨酸酶的抑制活性。结果设计、合成了18个新型的吡咯烷类化合物,其结构经核磁共振氢谱及质谱确定,并发现了几个具有较好活性的化合物。结论吡咯烷类化合物对神经氨酸酶有较高的抑制活性,值得进一步研究。
Abstract
OBJECTIVE To synthesize a series of novel pyrrolidine derivatives as neuraminidase inhibitors and test their inhibitory activities against neuraminidase.METHODS A series of pyrrolidine derivatives were synthesized from L-hydroxyproline,and the neuraminidase inhibitory activities of these compounds were tested using high throughput screening.RESULRS 18 Pyrrolidine derivatives were designed and synthesized.The basic structures of these compounds were verified by 1H-NMR and MS.Several compounds exhibited potent neuraminidase inhibitory activities.CONCLUSION Pyrrolidine derivatives exhibited potent neuraminidase inhibitory activities,and is worth of further investigation.
关键词
吡咯烷 /
神经氨酸酶 /
抑制剂 /
流感病毒 /
活性研究
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Key words
pyrrolidine /
neuraminidase /
inhibitor /
influenza virus
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张杰;王强;徐文方;刘艾林;杜冠华.
吡咯烷类神经氨酸酶抑制剂的设计、合成与初步活性研究[J]. 中国药学杂志, 2008, 43(04): 314-318
ZHNG Jie;WNG Qing;XU Wen-fng;LIU i-lin;DU Gun-hu.
Design,Synthesis,and Activity Study of Pyrrolidine Derivatives as Neuraminidase Inhibitors [J]. Chinese Pharmaceutical Journal, 2008, 43(04): 314-318
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参考文献
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脚注
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基金
国家自然科学基金资助项目(36072541)
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