| Discovery of novel 1-phenyl-cycloalkane carbamides as potent and selective influenza fusion inhibitors. | |
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MedLine Citation:
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PMID: 20494579 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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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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Publication Detail:
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Type: Journal Article Date: 2010-05-05 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 20 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2010 Jun |
Date Detail:
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Created Date: 2010-06-04 Completed Date: 2010-09-13 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 3507-10 Citation Subset: IM |
Copyright Information:
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Copyright 2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Roche R&D Center China, Shanghai, China. gordon.tang@roche.com |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Cell Line Cycloparaffins / chemistry, pharmacology*, therapeutic use Dogs Drug Discovery Hemagglutinin Glycoproteins, Influenza Virus / drug effects* Humans Influenza A Virus, H1N1 Subtype / drug effects* Influenza, Human / drug therapy Structure-Activity Relationship Urea / chemistry, pharmacology*, therapeutic use |
| Chemical | |
Reg. No./Substance:
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0/Cycloparaffins; 0/Hemagglutinin Glycoproteins, Influenza Virus; 57-13-6/Urea |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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