Počet záznamů: 1
New prodrugs of Adefovir and Cidofovir
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SYSNO ASEP 0360524 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název New prodrugs of Adefovir and Cidofovir Tvůrce(i) 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, ORCIDCelkový počet autorů 7 Zdroj.dok. Bioorganic & Medicinal Chemistry. - : Elsevier - ISSN 0968-0896
Roč. 19, č. 11 (2011), s. 3527-3539Poč.str. 13 s. Jazyk dok. eng - angličtina Země vyd. GB - Velká Británie Klíč. slova adefovir ; cidofovir ; antivirals ; prodrugs ; acyclic nucleoside phosphonate ; phosphonate ester ; in vitro evaluation Vědní obor RIV CC - Organická chemie CEP 1M0508 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000290955400028 DOI 10.1016/j.bmc.2011.04.016 Anotace 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. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Rok sběru 2012
Počet záznamů: 1