The Design, Synthesis and Antiviral Evaluation of a Series of 5-trimethylsilyl-1-β-d-(arabinofuranosyl) uracil phosphoramidate ProTides
Author(s) -
Youcef Mehellou,
Jan Balzarini,
Christopher McGuigan
Publication year - 2010
Publication title -
antiviral chemistry and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.919
H-Index - 51
eISSN - 2040-2066
pISSN - 0956-3202
DOI - 10.3851/imp1476
Subject(s) - phosphoramidate , uracil , nucleoside , uridine , nucleoside analogue , chemistry , biochemistry , herpes simplex virus , trimethylsilyl , virus , stereochemistry , biology , rna , virology , dna , organic chemistry , gene
Nucleoside analogues always require phosphorylation to be active. This appears to be a particular limitation for uridine-based nucleosides. Our ProTide method allows the direct use of masked membrane-soluble preformed nucleoside phosphates, bypassing the need for the initial phosphorylation step. We herein applied it to some novel 5-trimethylsilyl arabinosyl uridines.
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