| Synthesis of novel 6'-spirocyclopropyl-5'-norcarbocyclic adenosine phosphonic Acid analogues as potent anti-hiv agents. | |
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MedLine Citation:
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PMID: 21967289 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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Novel 5'-norcarbocyclic adenosine phosphonic acid analogues with 6'-electropositive moiety such as spirocyclopropane were designed and synthesized from the commercially available diethylmalonate 5. Regioselective Mitsunobu reaction proceeded in the presence of an allylic functional group at a low reaction temperature in polar cosolvent [dimethylformamide (DMF)/1,4-dioxane] to give purine analogue 15. To improve cellular permeability and enhance the anti-human immunodeficiency virus (HIV) activity of this phosphonic acid, a SATE phosphonodiester nucleoside prodrug 23 was prepared. The synthesized adenosine phosphonic acids analogues 18-21 and 23 were subjected to antiviral screening against HIV-1. |
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Authors:
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Lian Jin Liu; Eunae Kim; Joon Hee Hong |
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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: 30 ISSN: 1532-2335 ISO Abbreviation: Nucleosides Nucleotides Nucleic Acids Publication Date: 2011 Oct |
Date Detail:
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Created Date: 2011-10-04 Completed Date: - Revised Date: - |
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: 784-97 Citation Subset: IM |
Affiliation:
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a BK-21 Project Team, College of Pharmacy, Chosun University , Kwangju , Republic of Korea. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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