Are 5′- O-Carbamate-2′,3′-dideoxythiacytidine New Anti-HIV and Anti-HBV nucleoside Drugs or Prodrugs?

In contrast to 5′- O-carbonate 3TC derivatives ( 23, 24), which are clearly 3TC prodrugs, the corresponding 3TC carbamates ( 15– 21 and 25), found to be very stable compounds with respect to enzymatic hydrolysis (cellular lysates and culture cell media) and still active on both HIV-1 and HBV infecte...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2003-08, Vol.13 (15), p.2459-2463
Hauptverfasser: Anastasi, Carole, Vlieghe, Patrick, Hantz, Olivier, Schorr, Olivier, Pannecouque, Christophe, Witvrouw, Myriam, De Clercq, Erik, Clayette, Pascal, Dereuddre-Bosquet, Nathalie, Dormont, Dominique, Gondois-Rey, Françoise, Hirsch, Ivan, Kraus, Jean-Louis
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Sprache:eng
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Zusammenfassung:In contrast to 5′- O-carbonate 3TC derivatives ( 23, 24), which are clearly 3TC prodrugs, the corresponding 3TC carbamates ( 15– 21 and 25), found to be very stable compounds with respect to enzymatic hydrolysis (cellular lysates and culture cell media) and still active on both HIV-1 and HBV infected cells, may not be 3TC prodrugs. The antiviral properties as well as the mechanism of action of 3TC analogues have been studied and evaluated. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00496-7