Discovery of novel 1-phenyl-cycloalkane carbamides as potent and selective influenza fusion inhibitors |
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| Authors: | Guozhi Tang Zongxing Qiu Xianfeng Lin Wentao Li Lei Zhu Shaohua Li Haodong Li Lisha Wang Li Chen Jim Z. Wu Wengang Yang |
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| Affiliation: | 1. Roche R&D Center China, Shanghai 201203, China;2. WuXi Apptec Co., Ltd, Shanghai 200131, China |
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| 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 EC50 of 98 nM against H1N1 A/Weiss/43 strain and over 1000-fold selectivity against host MDCK cells. |
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