Nucleosides, Nucleotides & Nucleic Acids 2010-03-01

Design and synthesis of novel SATE derivatives of acyclic isocytosine and 9-deazaadenine C-nucleosides.

Lian Jin Liu, Joon Hee Hong

Index: Nucleosides Nucleotides Nucleic Acids 29(3) , 257-66, (2010)

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Abstract

This article describes a very simple route for synthesizing novel lipophilic phosphate bis(t-bu-SATE) prodrugs of acyclic cyclobutylated C-nucleosides such as isocytosine 12 and 9-deazaadenine 19, which were prepared from 1,1-gem cyclobutyl dicarboxylate. Synthesized compounds were evaluated as potential antiviral agents against HIV virus. Some phosphate SATE prodrugs were more active against HIV than parent nucleosides.