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ID: ALA1158631

Journal: Bioorg Med Chem Lett

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

Authors: Tang G, Qiu Z, Lin X, Li W, Zhu L, Li S, Li H, Wang L, Chen L, Wu JZ, Yang W.

Abstract: 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.

CiteXplore: 20494579

DOI: 10.1016/j.bmcl.2010.04.141