期刊
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
卷 31, 期 4, 页码 293-318出版社
TAYLOR & FRANCIS INC
DOI: 10.1080/15257770.2012.662611
关键词
Phosphonylated nucleosides; azidophosphonates; 1,3-dipolar cycloaddition 1,4-disubstituted-1,2,3-triazoles; phosphonic acid
资金
- National Science Centre [UMO-2011/01/D/NZ4/01276]
- K.U. Leuven (GOA) [10/014]
The 1,3-dipolar cycloaddition of diethyl 2-azidoethyl-, 3-azidopropyl-, 2-azido-1-hydroxyethyl-, 3-azido-2-hydroxypropylphosphonates with selected N-propargyl nucleobases gave a series of the phosphonylated 1,2,3-triazole acyclonucleosides in which the phosphonate residue and nucleobases were linked by three-and four-carbon chains. Under standard conditions (TMSBr, ethanol), all synthesized O,O-diethylphosphonates were transformed into the respective phosphonic acids. All compounds were evaluated in vitro for activity against a broad variety of DNA and RNA viruses. Unfortunately, no antiviral activity was observed at 100 mu M.
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