金刚烷胺
三环
连接器
铅化合物
病毒
IC50型
化学
甲型流感病毒
立体化学
结构-活动关系
病毒学
组合化学
药理学
生物
生物化学
体外
计算机科学
操作系统
作者
Jing Jiang,Xiao-Qiang Zhao,Tianyu Niu,Haiyan Yan,L I Yinghong,L I Yuhuan,Dan–Qing Song,Sheng Tang,Jianguo Xing
出处
期刊:PubMed
日期:2019-05-01
卷期号:74 (5): 265-269
摘要
A series of new matrinic derivatives with an 11-adamantyl group were designed, synthesized and evaluated for their anti-influenza A H3N2 activities, based on the privileged structure strategy.SAR analysis indicated that introduction of an 11-adamantyl by ester linker might be helpful for the activity. Among them, compound 7b exhibited promising anti-H3N2 activities with IC50 value of 5.14 μM, slightly better than that of amantadine. Its activity was further confirmed at the protein level. In primary mechanism, compound 7b could inhibit virus replication cycle at early stage by targeting M2 protein, consistent with that of amantadine. This study represents a successful application of combined strategy of privileged amantadine segment for further structural optimization and development of a new class of anti-influenza agents.
科研通智能强力驱动
Strongly Powered by AbleSci AI