Synthesis and evaluation of anti-HIV activity of 3-azido-4-(hydroxymethyl)tetrahydrofuran derivatives containing 2-(thymin-1-yl)methyl, 2-(cytosin-1-yl)methyl or 2-(adenin-9-yl)methyl substituents – a new series of AZT analogues

摘要

The three monocyclic AZT analogues 6, 7 and 8 {3-azido-4-(hydroxymethyl)tetrahydrofuran derivatives containingn2-[(thymin-1-yl)methyl], 2-[(cytosin-1-yl)methyl] and 2-[(adenin-9-yl)methyl] substituents} are synthesized via methyln3-azido-3-deoxy-2-O,4-C-methylene--ribofuranoside 13 as key intermediate. All nucleoside analogues proved to bendevoid of anti-HIV activity in MT-4 cells.