title: Discovery of highly potent agents against influenza A virus.
abstract: We previously reported several new M2 inhibitors as active as amantadine against influenza A virus and validated by three types of in vitro assays. Herein, we further modified one of the most potent hits in a viral inhibition assay and conducted structure-activity relationship studies on this scaffold. As a result, compound 8e was identified to be the most potent inhibitor against wild-type influenza A virus, being nearly 240-fold more active than amantadine.
authors.affiliation: Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, 190 Kai Yuan Avenue, Guangzhou Science Park, Guangzhou 510530, People's Republic of China.
authors.forename: Xin
authors.initials: X
authors.lastname: Zhao
authors.forename: Chufang
authors.initials: C
authors.lastname: Li
authors.forename: Shaogao
authors.initials: S
authors.lastname: Zeng
authors.forename: Wenhui
authors.initials: W
authors.lastname: Hu
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004285:Dogs; D055808:Drug Discovery / Q000379:methods*; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects / Q000254:growth & development; D053122:Influenza A Virus, H3N2 Subtype / Q000187:drug effects / Q000254:growth & development; D009980:Influenza A virus / Q000187:drug effects* / Q000254:growth & development; D013329:Structure-Activity Relationship; D014763:Viral Matrix Proteins / Q000037:antagonists & inhibitors; D010948:Viral Plaque Assay; D000086082:Viroporin Proteins
chemical_list: D000998:Antiviral Agents; D014763:Viral Matrix Proteins; C488937:M2 protein, Influenza A virus; D000086082:Viroporin Proteins