Title: Enhancing the aqueous solubility of d4T-based phosphoramidate prodrugs
Authors: Siddiqui, A ×
McGuigan, C
Ballatore, C
Srinivasan, S
De Clercq, Erik
Balzarini, Jan #
Issue Date: 27-May-2000
Series Title: Bioorganic & medicinal chemistry letters vol:10 issue:4 pages:381-4
Abstract: A range of polyether para-substituted phosphoramidates were synthesised and found to have substantially elevated aqueous solubilities compared to the underivatised parent prodrug. A 30-fold increase in aqueous solubility could be achieved without a substantial decrease of in vitro activity against HIV-1. Replacement of the aryl (i.e. phenolic) moiety by tyrosine led to a substantial enhancement in aqueous solubility but also to a decrease in antiviral potency. A previously unobserved trend was identified, relating increased aryl substituent steric bulk to decreased antiviral activity.
ISSN: 0960-894X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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