Anti-flavivirus Activity of Different Tritylated Pyrimidine and Purine Nucleoside Analogues

作者:McGuigan Christopher*; Serpi Michaela; Slusarczyk Magdalena; Ferrari Valentina; Pertusati Fabrizio; Meneghesso Silvia; Derudas Marco; Farleigh Laura; Zanetta Paola; Bugert Joachim
来源:ChemistryOpen, 2016, 5(3): 227-235.
DOI:10.1002/open.201500216

摘要

A series of tritylated and dimethoxytritylated analogues of selected pyrimidine and purine nucleosides were synthesized and evaluated for their in vitro inhibitory activity against two important members of the genus Flavivirus in the Flaviviridae family, the yellow fever (YFV) and dengue viruses (DENV). Among all compounds tested, the 5 '-O-tritylated and the 5 '-O-dimethoxytritylated 5-fluorouridine derivatives exerted potency against YFV. Interestingly in the series of purine analogues, the 5 ' O, N-bis-tritylated fludarabine derivative revealed strong inhibitory activity against DENV at mu m concentrations, however significantly weaker potency against YFV.

  • 出版日期2016-6