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通过对小的伯胺库的有针对性筛选,鉴定基质 2 蛋白抑制剂。

Identification of hits as matrix-2 protein inhibitors through the focused screening of a small primary amine library.

机构信息

Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou Science Park, Guangdong 510530, People's Republic of China.

出版信息

J Med Chem. 2010 May 13;53(9):3831-4. doi: 10.1021/jm901664a.

Abstract

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.

摘要

虽然金刚烷衍生物是抗甲型流感病毒的唯一 M2 药物,但由于耐药性,它们在美国的使用受到限制。在这里,我们报告了通过使用基于金刚烷的支架跳跃策略设计的小型初级胺文库的重点筛选快速产生的多种 M2 抑制剂的鉴定。这些化合物与金刚烷一样有效,可能是进一步产生先导化合物过程的候选物。

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