Discovery of novel 1-phenyl-cycloalkane carbamides as potent and selective influenza fusion inhibitors.
Tang G, Qiu Z, Lin X, Li W, Zhu L, Li S, Li H, Wang L, Chen L, Wu JZ, Yang W.
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.