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New prodrugs of Adefovir and Cidofovir

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F11%3A00360524" target="_blank" >RIV/61388963:_____/11:00360524 - isvavai.cz</a>

  • Result on the web

    <a href="http://dx.doi.org/10.1016/j.bmc.2011.04.016" target="_blank" >http://dx.doi.org/10.1016/j.bmc.2011.04.016</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.bmc.2011.04.016" target="_blank" >10.1016/j.bmc.2011.04.016</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    New prodrugs of Adefovir and Cidofovir

  • Original language description

    New Adefovir (PMEA) prodrugs with a pro-moiety consisting of decyl(oxyethyl) chain bearing hydroxyl function(s), hexaethyleneglycol or a (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl unit were prepared from the tetrabutylammonium salt of the phosphonate drugand an appropriate alkyl bromide or tosylate. Analogously, two esters of Cidofovir [(S)-HPMPC] bearing a hexaethyleneglycol moiety were prepared. The antiviral activity of the prodrugs was evaluated in vitro. A loss in the antiviral activities of the hydroxylated decyl(oxyethyl) esters and hexaethyleneglycol esters of PMEA against HIV and herpesviruses occurred in comparison with the parent compound. On the other hand, the (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl ester of PMEA showed significant activities against HIV and herpesviruses. (S)-HPMPC prodrugs exhibited anti-cytomegalovirus activities in the same range as the parent drug, whereas the anti-HSV and anti-VZV activities were one- to seven-fold lower than that of Cidofovir.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    CC - Organic chemistry

  • OECD FORD branch

Result continuities

  • Project

    <a href="/en/project/1M0508" target="_blank" >1M0508: New Antivirals and Antineoplastics</a><br>

  • Continuities

    Z - Vyzkumny zamer (s odkazem do CEZ)

Others

  • Publication year

    2011

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Bioorganic & Medicinal Chemistry

  • ISSN

    0968-0896

  • e-ISSN

  • Volume of the periodical

    19

  • Issue of the periodical within the volume

    11

  • Country of publishing house

    GB - UNITED KINGDOM

  • Number of pages

    13

  • Pages from-to

    3527-3539

  • UT code for WoS article

    000290955400028

  • EID of the result in the Scopus database