- Synthesis and antiviral activity of C-5 substituted analogues of d4T bearing methylamino- or methyldiamino-linker arms
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A general strategy is reported for the preparation of C-5-methylamino- or methyldiamino-d4t analogues of 'different sizes'. Reactions of the 2',3'- didehydro-2',3'-dideoxy-C-5 hydroxymethyl precursor (7) with either polymethylene diamines (n = 6, 8, 10 and 12) or propargylamine proceed regioselectively via substitution reactions at the C-5 position of uracil. The compounds were evaluated for antiviral activity and cytotoxicity. No significant activity was observed for compounds 9, 11, and 13, but 10 and 12 exhibited a weak activity against HIV-1.
- Gavriliu,Fossey,Fontaine,Benzaria,Ciurea,Delbederi,Lelong,Laduree,Aubertin,Kirn
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- Alternative synthetic routes to 2′,3′-didehydro-2′,3′-dideoxy-5-hydroxymethyluridine
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Alternative syntheses for the nucleoside analogue 2′,3′-didehydro-2′,3′-dideoxy-5-hydroxymethyluridine starting from 5-methyluridine and uridine are described.
- Chung, Raymond,Anderson, Karen S.
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p. 8361 - 8363
(2007/10/03)
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