流感病毒神经氨酸酶抑制剂的合成筛选

Screening and synthesis of influenza neuraminidase inhibitors

总结流感神经氨酸酶抑制剂有效的结构特点及其结晶结构 ,对神经氨酸酶抑制剂进行了合成探索和构效关系研究 ,共设计合成 6个未见报道的新化合物 ,其中 3个为目标物 ,3个为中间体 ,通过MS ,1 H NMR证明其结构 ,并测定了它们的抑酶活性 ,结果所有化合物对神经氨酸酶都显示一定活性。同时还测定了这几个化合物抗流感病毒株粤防 72 2 4 3的活性及体外抗HIV 1整合酶活性。

On the basis of effective structural feature and crystal structure of the neuraminidase inhibitors, some research on the synthesis and structure activity relationship of neuraminidase inhibitors was conducted. Six new compounds have been prepared in the study, including three intermediates and three target compounds. All compounds synthesized were verified by 1 H NMR and MS. They all had some effects against neuraminidase, and the activity against virus YueFang 72 243 in vitro was also studied.