tetano
Editor, Senior Moderator
Bioorg Med Chem Lett. 2010 May 5. [Epub ahead of print]
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.
Roche R&D Center China, Shanghai 201203, China.
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 98nM against H1N1 A/Weiss/43 strain and over 1000-fold selectivity against host MDCK cells. Copyright ? 2010 Elsevier Ltd. All rights reserved.
PMID: 20494579 [PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/20494579
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.
Roche R&D Center China, Shanghai 201203, China.
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 98nM against H1N1 A/Weiss/43 strain and over 1000-fold selectivity against host MDCK cells. Copyright ? 2010 Elsevier Ltd. All rights reserved.
PMID: 20494579 [PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/20494579