含氟无环核苷及其磷酰胺酯的合成与抗病毒活性评价
Synthesis and antiviral evaluation of fluorinated acyclo-nucleosides and their phosphoramidates.
作者信息
Mahmoud Sawsan, Li Hao, McBrayer Tamara R, Bassit Leda, Hammad Sherif F, Coats Steven J, Amblard Franck, Schinazi Raymond F
机构信息
a Center for AIDS Research , Laboratory of Biochemical Pharmacology , Department of Pediatrics , Emory University School of Medicine , Atlanta , Georgia , USA.
b Department of Pharmaceutical Chemistry , Faculty of Pharmacy, Helwan University , Helwan , Egypt.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2017 Jan 2;36(1):66-82. doi: 10.1080/15257770.2016.1218023. Epub 2016 Oct 19.
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.
摘要
从市售的2,2,3,3-四氟-1,4-丁二醇和2,2,3,3,4,4-六氟-1,5-戊二醇出发，通过四到六步反应成功制备了一系列新型的四氟和六氟无环核苷及其氨基磷酸酯。评估了它们阻断HIV、HCV、HSV-1和HBV复制的能力以及它们对HepG2、人淋巴细胞、CEM和Vero细胞的细胞毒性。
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