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
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CC - Organic chemistry
OECD FORD branch
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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
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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
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