Source:http://linkedlifedata.com/resource/pubmed/id/21565516
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
11
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pubmed:dateCreated |
2011-5-25
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pubmed:abstractText |
New Adefovir (PMEA) prodrugs with a pro-moiety consisting of decyl or decyloxyethyl chain bearing hydroxyl function(s), hexaethyleneglycol or a (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl unit were prepared starting from the tetrabutylammonium salt of the phosphonate drug and an appropriate alkyl bromide or tosylate. Analogously, two esters of Cidofovir [(S)-HPMPC] bearing a hexaethyleneglycol moiety were prepared. The activity of the prodrugs was evaluated in vitro against different virus families. A loss in the antiviral activities of the hydroxylated decyl or decyloxyethyl esters and hexaethyleneglycol esters of PMEA against human immunodeficiency virus (HIV) and herpesviruses [including herpes simplex virus (HSV), varicella-zoster virus (VZV), and human cytomegalovirus (CMV)] 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.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Adenine,
http://linkedlifedata.com/resource/pubmed/chemical/Antiviral Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cytosine,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphonic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Prodrugs,
http://linkedlifedata.com/resource/pubmed/chemical/adefovir,
http://linkedlifedata.com/resource/pubmed/chemical/cidofovir
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3527-39
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pubmed:meshHeading |
pubmed-meshheading:21565516-Adenine,
pubmed-meshheading:21565516-Animals,
pubmed-meshheading:21565516-Antiviral Agents,
pubmed-meshheading:21565516-Cell Line, Tumor,
pubmed-meshheading:21565516-Cytomegalovirus,
pubmed-meshheading:21565516-Cytosine,
pubmed-meshheading:21565516-HIV,
pubmed-meshheading:21565516-Herpesvirus 3, Human,
pubmed-meshheading:21565516-Humans,
pubmed-meshheading:21565516-Phosphonic Acids,
pubmed-meshheading:21565516-Prodrugs,
pubmed-meshheading:21565516-Simplexvirus
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pubmed:year |
2011
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pubmed:articleTitle |
New prodrugs of Adefovir and Cidofovir.
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pubmed:affiliation |
Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Prague 166 10, Czech Republic. tichy78@uochb.cas.cz
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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