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QIU Jingying, HU Zhanxing, XU Bixue, PAN Weidong, HUANG Zhengming, LIU Changxiao, LIANG Guangyi. Synthesis and anti-HBV activity evaluation of Matijin-Su derivatives with aromatic heterocycles[J]. Journal of China Pharmaceutical University, 2015, 46(6): 641-646. DOI: 10.11665/j.issn.1000-5048.20150601
Citation: QIU Jingying, HU Zhanxing, XU Bixue, PAN Weidong, HUANG Zhengming, LIU Changxiao, LIANG Guangyi. Synthesis and anti-HBV activity evaluation of Matijin-Su derivatives with aromatic heterocycles[J]. Journal of China Pharmaceutical University, 2015, 46(6): 641-646. DOI: 10.11665/j.issn.1000-5048.20150601
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Synthesis and anti-HBV activity evaluation of Matijin-Su derivatives with aromatic heterocycles

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  • Hepatitis B virus(HBV)-infected hepatitis is one of the most common infectious disease worldwide. To find novel effective anti-HBV agents, a series of Matijin-Su(MTS)derivatives with aromatic heterocycles were synthesized and evaluated for their anti- HBV activities in HepG2 2. 2. 15 cells. Among them, compounds 7a( IC50=2. 94 μmol/L)and 9a( IC50=2. 21 μmol/L)exhibited more potent inhibitory activity against the replication of HBV DNA in HepG2 2. 2. 15 cells than that of lead compound MTS(IC50=11. 16 μmol/L). Notably, both 7a and 9a displayed a high selective index(SI)of 146. 39 and > 250, respectively, which were also much higher than that of MTS(SI=10. 78). Therefore, compounds 7a and 9a may be promising anti-HBV agents with safety profile for HBV infection.
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