Cytosine deoxyribonucleoside anti-HIV analogues : a small chemical substitution allows relevant activities
Articolo
Data di Pubblicazione:
2012
Citazione:
Cytosine deoxyribonucleoside anti-HIV analogues : a small chemical substitution
allows relevant activities / F. Scaglione, L. Berrino. - In: INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS. - ISSN 0924-8579. - 39:6(2012 Jun), pp. 458-463.
Abstract:
The search for new nucleoside analogue compounds targeting the virally encoded reverse transcriptase was developed by modifying the nucleoside structure to create inhibitor compounds. In this review, the structure-activity relationship of antiviral compounds synthesised from the naturally existing cytosine deoxyribonucleoside (dC) was evaluated. The line of research starting from dC led to the synthesis of 2',3'-dideoxycytidine (ddC; zalcitabine), 2',3'-dideoxy-3'-thiacytidine (3TC; lamivudine) and 2',3'-dideoxy-5-fluoro-3'-thiacytidine (FTC; emtricitabine) and looks very interesting because each product comes from a single small change in the chemical structure of the former compound, resulting in a progressive improvement in terms of activity, pharmacokinetics, tolerability and emergence of resistance.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Zalcitabine ; Lamivudine ; Emtricitabine
Elenco autori:
F. Scaglione, L. Berrino
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