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

Wenhui Hu; Shaogao Zeng; Chufang Li; Yanling Jie; Zhiyuan Li; Ling Chen

doi:10.1021/jm901664a

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.

Authors

Wenhui Hu¹, Shaogao Zeng, Chufang Li, Yanling Jie, Zhiyuan Li, Ling Chen

Affiliation

¹ Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou Science Park, Guangdong 510530, People's Republic of China. [email protected]

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Amantadine / pharmacology
Amines / pharmacology*
Antiviral Agents / chemistry*
Antiviral Agents / pharmacology
Drug Design
Drug Evaluation, Preclinical
Drug Resistance, Viral
Influenza A virus / drug effects*
Small Molecule Libraries
Viral Matrix Proteins / antagonists & inhibitors*

Substances

Amines
Antiviral Agents
M2 protein, Influenza A virus
Small Molecule Libraries
Viral Matrix Proteins
Amantadine