Identification of Hits as Matrix-2 Protein Inhibitors through the Focused Screening of a Small Primary Amine Library

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• 作者：Wenhui Hu ; Shaogao Zeng ; Chufang Li ; Yanling Jie ; Zhiyuan Li ; Ling Chen
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：May 13, 2010
• 年：2010
• 卷：53
• 期：9
• 页码：3831-3834
• 全文大小：726K
• 年卷期：v.53,no.9(May 13, 2010)
• ISSN：1520-4804

文摘

Although amantadine derivatives are the only M2 drugs for influenza virus A, their use is limited in the U.S. because of drug resistance. Here we report the identification of multiple M2 inhibitors that were rapidly generated through focused screening of a small primary amine library that was designed using a scaffold-hopping strategy based on amantadine. These compounds are as active as amantadine and might be hits for further lead generation processes.