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New prodrugs of Adefovir and Cidofovir
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SYSNO ASEP 0360524 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title New prodrugs of Adefovir and Cidofovir Author(s) Tichý, Tomáš (UOCHB-X) RID
Andrei, G. (BE)
Dračínský, Martin (UOCHB-X) RID, ORCID
Holý, Antonín (UOCHB-X)
Balzarini, J. (BE)
Snoeck, R. (BE)
Krečmerová, Marcela (UOCHB-X) RID, ORCIDNumber of authors 7 Source Title Bioorganic & Medicinal Chemistry. - : Elsevier - ISSN 0968-0896
Roč. 19, č. 11 (2011), s. 3527-3539Number of pages 13 s. Language eng - English Country GB - United Kingdom Keywords adefovir ; cidofovir ; antivirals ; prodrugs ; acyclic nucleoside phosphonate ; phosphonate ester ; in vitro evaluation Subject RIV CC - Organic Chemistry R&D Projects 1M0508 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000290955400028 DOI 10.1016/j.bmc.2011.04.016 Annotation 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 drug and 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Year of Publishing 2012
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