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L-beta-(2S,4S)- and L-alpha-(2S,4R)-dioxolanyl nucleosides as potential anti-HIV agents: asymmetric synthesis and structure-activity relationships.
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Affinity of the antiviral enantiomers of oxathiolane cytosine nucleosides for human 2'-deoxycytidine kinase.氧硫杂环戊烷胞嘧啶核苷的抗病毒对映体对人2'-脱氧胞苷激酶的亲和力。
Biochem Pharmacol. 1993 Apr 6;45(7):1540-3. doi: 10.1016/0006-2952(93)90058-5.
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Antiviral activity of 2',3'-dideoxy-beta-L-5-fluorocytidine (beta-L-FddC) and 2',3'-dideoxy-beta-L-cytidine (beta-L-ddC) against hepatitis B virus and human immunodeficiency virus type 1 in vitro.2',3'-二脱氧-β-L-5-氟胞苷（β-L-FddC）和2',3'-二脱氧-β-L-胞苷（β-L-ddC）在体外对乙型肝炎病毒和1型人类免疫缺陷病毒的抗病毒活性。
Biochem Pharmacol. 1994 Jan 20;47(2):171-4. doi: 10.1016/0006-2952(94)90002-7.
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Chronic viral hepatitis: diagnosis and management.慢性病毒性肝炎：诊断与管理
Hosp Pract (Off Ed). 1994 Feb 15;29(2):117-20, 123-6, 129-32. doi: 10.1080/21548331.1994.11442979.
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Anti-human immunodeficiency virus activities of the beta-L enantiomer of 2',3'-dideoxycytidine and its 5-fluoro derivative in vitro.2',3'-双脱氧胞苷的β-L对映体及其5-氟衍生物的体外抗人免疫缺陷病毒活性
Antimicrob Agents Chemother. 1994 Jun;38(6):1292-7. doi: 10.1128/AAC.38.6.1292.
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Enantiomeric 2',3'-dideoxycytidine derivatives are potent human immunodeficiency virus inhibitors in cell cultures.对映体2'，3'-双脱氧胞苷衍生物在细胞培养物中是有效的人类免疫缺陷病毒抑制剂。
C R Acad Sci III. 1994 Jan;317(1):85-9.
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Characterization of human immunodeficiency viruses resistant to oxathiolane-cytosine nucleosides.对奥沙硫杂环戊烷胞嘧啶核苷耐药的人类免疫缺陷病毒的特性分析
Antimicrob Agents Chemother. 1993 Apr;37(4):875-81. doi: 10.1128/AAC.37.4.875.
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Influence of stereochemistry on antiviral activities and resistance profiles of dideoxycytidine nucleosides.立体化学对双脱氧胞苷核苷抗病毒活性及耐药性的影响。
Antimicrob Agents Chemother. 1994 Apr;38(4):868-71. doi: 10.1128/AAC.38.4.868.
9
No effect of zidovudine on hepatitis B virus replication in homosexual men with symptomatic HIV-1 infection.齐多夫定对有症状HIV-1感染的同性恋男性体内乙肝病毒复制无影响。
AIDS. 1991 Feb;5(2):217-20. doi: 10.1097/00002030-199102000-00014.
10
Use of a standardized cell culture assay to assess activities of nucleoside analogs against hepatitis B virus replication.使用标准化细胞培养试验评估核苷类似物对乙型肝炎病毒复制的活性。
Antiviral Res. 1992 Jul 1;19(1):55-70. doi: 10.1016/0166-3542(92)90056-b.

β-2',3'-二脱氧胞苷类似物的纯核苷对映体在体外是乙型肝炎病毒的选择性抑制剂。

Pure nucleoside enantiomers of beta-2',3'-dideoxycytidine analogs are selective inhibitors of hepatitis B virus in vitro.

作者信息

Schinazi R F, Gosselin G, Faraj A, Korba B E, Liotta D C, Chu C K, Mathé C, Imbach J L, Sommadossi J P

机构信息

Georgia VA Research Center for AIDS and HIV Infections, Veterans Affairs Medical Center, Decatur 30033.

出版信息

Antimicrob Agents Chemother. 1994 Sep;38(9):2172-4. doi: 10.1128/AAC.38.9.2172.

DOI:10.1128/AAC.38.9.2172
PMID:7811039
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC284704/
Abstract

(-)-beta-L-2',3'-Dideoxycytidine (beta-L-DDC), (+)-beta-D-2',3'-dideoxycytidine (beta-D-DDC), (-)-beta-L-2',3'-dideoxy-5-fluorocytidine (beta-L-FDDC), (-)-beta-L-2',3'-dideoxy-5-fluoro-3'-thiacytidine (beta-L-FTC), and (+)-beta-D-1,3-dioxolane-5-fluorocytidine (beta-D-FDOC) were evaluated for their anti-hepatitis B virus (anti-HBV) activities in HBV-transfected human liver cells (2.2.15). The order of decreasing potency for the compounds at the 90% effect level was beta-D-FDOC > beta-L-FTC > beta-L-FDDC approximately beta-L-DDC >> beta-D-DDC. Inhibition of HBV in transfected liver cells by the cytosine nucleosides was selective. The beta-L-nucleoside-5'-triphosphates were consistently more potent inhibitors of woodchuck hepatitis virus DNA polymerase than the corresponding natural beta-D-enantiomers.

摘要

对（-）-β-L-2'，3'-二脱氧胞苷（β-L-DDC）、（+）-β-D-2'，3'-二脱氧胞苷（β-D-DDC）、（-）-β-L-2'，3'-二脱氧-5-氟胞苷（β-L-FDDC）、（-）-β-L-2'，3'-二脱氧-5-氟-3'-硫代胞苷（β-L-FTC）和（+）-β-D-1，3-二氧戊环-5-氟胞苷（β-D-FDOC）在乙肝病毒（HBV）转染的人肝细胞（2.2.15）中进行了抗乙肝病毒（抗HBV）活性评估。在90%效应水平下，这些化合物效力递减顺序为β-D-FDOC＞β-L-FTC＞β-L-FDDC≈β-L-DDC＞＞β-D-DDC。胞嘧啶核苷对转染肝细胞中HBV的抑制具有选择性。β-L-核苷-5'-三磷酸作为土拨鼠肝炎病毒DNA聚合酶抑制剂始终比相应的天然β-D-对映体更有效。