ISSN 0235-7216
ISSN 2424-4538 (online)
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2015 m. Nr. 2
Synthesis of novel derivatives of 5-carboxyuracil
Daiva TAURAITĖ, Julija DABUŽINSKAITĖ, Rytis RAŽANAS, Jaunius URBONAVIČIUS, Jonita STANKEVIČIŪTĖ, Saulius SERVA, Rolandas MEŠKYS
The synthesis and characterization of 13 new 5-carboxyuracil derivatives bearing ester and amide groups is described. Five previously synthesised 5-carboxyuracil esters were prepared by a new procedure using carbodiimide as a coupling reagent. The prepared compounds were tested as inhibitors of DNA polymerases, particularly M. MuLV and HIV-1 reverse transcriptases. In addition, it is shown that the methyl, ethyl, propyl, isopropyl, butyl, cyclohexyl, cyclooctyl, and prop-2-ynyl esters of 5-carboxyuracil are substrates of thymidine phosphorylase, thus allowing enzymatic synthesis of novel modified nucleosides.
Keywords: 5-carboxyuracil, inhibition, reverse transcriptase, modified nucleosides
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