Discovery of novel 1-phenyl-cycloalkane carbamides as potent and selective influenza fusion inhibitors

作者：Tang Guozhi^*; Qiu Zongxing; Lin Xianfeng; Li Wentao; Zhu Lei; Li Shaohua; Li Haodong; Wang Lisha; Chen Li; Wu Jim Z; Yang Wengang

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(12): 3507-3510.

DOI：10.1016/j.bmcl.2010.04.141

• Influenza A
• Fusion inhibitor
• Hemagglutinin

A novel class of HA inhibitors (4a) was identified based on ligand similarity search of known HA inhibitors. Parallel synthesis and further structural modifications resulted in 1-phenyl-cyclopentanecarboxylic acid (4-cyano-phenyl)-methyl-amide 4t as a potent and selective inhibitor to phylogenetic H1 influenza viruses with an EC(50) of 98 nM against H1N1 A/Weiss/43 strain and over 1000-fold selectivity against host MDCK cells.

• 出版日期2010-6-15