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一種新型苯甲酸衍生物類神經(jīng)氨酸酶抑制劑的合成及體外酶抑制活性

發(fā)布時(shí)間:2019-05-20 13:55
【摘要】:本研究基于苯甲酸衍生物類神經(jīng)氨酸酶抑制劑的結(jié)構(gòu),依據(jù)最新報(bào)道的構(gòu)效關(guān)系設(shè)計(jì)了新的先導(dǎo)化合物 L,并合成4個(gè)未見文獻(xiàn)報(bào)道的苯甲酸衍生物類神經(jīng)氨酸酶抑制劑 ( Ⅰ~Ⅳ )。活性測(cè)試選用流感病毒菌株 H_3N_2( California/04)、H_1N_1(California/99) 和 B(Shanghai/02)。結(jié)果顯示,化合物Ⅰ~Ⅳ均具有良好的神經(jīng)氨酸酶抑制作用,含環(huán)狀分支的Ⅱ活性最佳。
[Abstract]:Based on the structure of the neuraminidase inhibitor of the benzoic acid derivatives, the new pilot compound L was designed according to the structure-effect relationship of the most recent reports, and 4 kinds of neuraminidase inhibitors (I-IV), which were not reported in the literature, were synthesized. The activity tests were influenza virus strain H _ 3N _ 2 (California/04), H _ 1N _ 1 (California/99) and B (Shanghai/02). The results showed that the compounds I to IV had good inhibitory effect on neuraminidase, and the 鈪,

本文編號(hào):2481693

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