【摘 要】
：
In recent years,the new influenza A(H1N1) virus and H5N1 avian influenza virus epidemic has a tremendous impact on human health.Up to now,the anti-influenza drugs were approved for clinical use,which
【机 构】
：
School of Pharmaceutical Sciences,Key lab of New drug screening in Guangdong province. Southern Medi
【出 处】
：
第五届岭南有机化学论坛暨华南理工大学-兰州大学有机化学双边论坛
论文部分内容阅读
In recent years,the new influenza A(H1N1) virus and H5N1 avian influenza virus epidemic has a tremendous impact on human health.Up to now,the anti-influenza drugs were approved for clinical use,which targeted only two drug proteins,the neuraminidase and M2 ion channel protein.All of the above drugs are faced with the increasingly serious problem of drug resistance.Therefore,it is needed urgently to explore the new mechanism anti-influenza drugs.We previously validated the conservative functional regions of influenza virus envelope protein hemagglutinin(HA) as new anti-influenza drug targets and found CL-385319 can inhibit A/Vietnam/1194/2004 H5N1 virus infection.Analysis of the conservative binding site that CL-385319 induced,we thought the binding of CL-385319 to HA is a process of "induced fit".Next,we further studied the structure optimization,structure activity relationship and mechanism of the lead compounds targeting the HA conserved region,result in better compounds with more potent compounds,including 1l,3sc and 4sc(Scheme 1).
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