Cytosine deoxyribonucleoside anti-HIV analogues: a small chemical substitution allows relevant activities.

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.

authors

Scaglione F,Berrino L

doi

10.1016/j.ijantimicag.2011.11.013

subject

Has Abstract

pub_date

2012-06-01 00:00:00

pages

458-63

issue

6

eissn

0924-8579

issn

1872-7913

pii

S0924-8579(12)00002-7

journal_volume

39

pub_type

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