Synthesis and antiviral evaluation of fluorinated acyclo-nucleosides and their phosphoramidates |
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Authors: | Sawsan Mahmoud Hao Li Tamara R. McBrayer Leda Bassit Sherif F. Hammad Steven J. Coats |
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Affiliation: | 1. Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia, USA;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Helwan, Egypt;3. CocrystalPharma, Inc., Tucker, Georgia, USA;4. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Helwan, Egypt |
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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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Keywords: | Fluorine acyclonucleoside phosphoramidates antiviral agent |
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