| Phosphoramidate protides of 2',3'-dideoxy-3'-fluoroadenosine and related nucleosides with potent activity against HIV and HBV. | |
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MedLine Citation:
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PMID: 14609234 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Syntheses of phosphoramidate protides of several 2',3'-dideoxy-3'-fluoroadenosine derivatives by treatment of the nucleoside with phosphorochloridates in the presence of pyridine and t-BuMgCl is described. Several of these protides showed significantly improved antiviral potency over the parent nucleoside against HIV and HBV. Especially marked was the improvement in potency of phosphoramidate protides of 2',3'-dideoxy-3'-fluoroadenosine against both HIV and HBV. |
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Authors:
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Kristjan S Gudmundsson; Susan M Daluge; Lance C Johnson; Robert Jansen; Richard Hazen; Lynn D Condreay; Christopher McGuigan |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Nucleosides, nucleotides & nucleic acids Volume: 22 ISSN: 1525-7770 ISO Abbreviation: Nucleosides Nucleotides Nucleic Acids Publication Date: 2003 Oct |
Date Detail:
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Created Date: 2003-11-11 Completed Date: 2004-06-21 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 100892832 Medline TA: Nucleosides Nucleotides Nucleic Acids Country: United States |
Other Details:
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Languages: eng Pagination: 1953-61 Citation Subset: IM |
Affiliation:
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Division of Chemistry, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA. Kristjan.S.Gudmundsson@gsk.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Amides
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chemistry* Antiviral Agents / chemical synthesis, chemistry*, pharmacology*, toxicity Cell Line, Tumor Deoxyadenosines / chemical synthesis*, chemistry, pharmacology*, toxicity Dideoxyadenosine / analogs & derivatives*, chemical synthesis, chemistry, pharmacology, toxicity HIV / drug effects* Hepatitis B virus / drug effects* Humans Inhibitory Concentration 50 Lymphocytes / cytology, drug effects, virology Molecular Structure Phosphoric Acids / chemistry* |
| Chemical | |
Reg. No./Substance:
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0/Amides; 0/Antiviral Agents; 0/Deoxyadenosines; 0/Phosphoric Acids; 2817-45-0/phosphoramidic acid; 4097-22-7/Dideoxyadenosine; 75059-22-2/3'-fluoro-3'-deoxyadenosine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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