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 |
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Hauptverfasser: | , , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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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.
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(03)00496-7 |