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

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

  • J Med Chem. 2010 May 13;53(9):3831-4. doi: 10.1021/jm901664a.
Wenhui Hu 1,  Shaogao Zeng,  Chufang Li,  Yanling Jie,  Zhiyuan Li,  Ling Chen
Affiliations

Affiliation

  • 1 Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou Science Park, Guangdong 510530, People's Republic of China. hu_wenhui@gibh.ac.cn
PMID: 20394375 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.

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