Synthesis and antiviral evaluation of fluorinated acyclo-nucleosides and their phosphoramidates

氟化无环核苷及其磷酰胺的合成及抗病毒评价

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作者:Sawsan Mahmoud, Hao Li, Tamara R McBrayer, Leda Bassit, Sherif F Hammad, Steven J Coats, Franck Amblard, Raymond F Schinazi

Abstract

A novel series of tetrafluoro and hexafluoro acyclic nucleosides and their phosphoramidates were successfully prepared from commercially available 2,2,3,3-tetrafluoro-1,4-butanediol and 2,2,3,3,4,4-hexafluoro-1,5-pentanediol in four to six steps. Their ability to block HIV, HCV, HSV-1, and HBV replication along with their cytotoxicity toward HepG2, human lymphocyte, CEM, and Vero cells was assessed.

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