• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

2'-脱氧-3'-硫代胞苷（BCH 189）的分离对映体在体外均能抑制人类免疫缺陷病毒的复制。

The separated enantiomers of 2'-deoxy-3'-thiacytidine (BCH 189) both inhibit human immunodeficiency virus replication in vitro.

作者信息

Coates J A, Cammack N, Jenkinson H J, Mutton I M, Pearson B A, Storer R, Cameron J M, Penn C R

机构信息

Department of Virology, Glaxo Group Research Ltd., Greenford, Middlesex, United Kingdom.

出版信息

Antimicrob Agents Chemother. 1992 Jan;36(1):202-5. doi: 10.1128/AAC.36.1.202.

DOI:10.1128/AAC.36.1.202
PMID:1590690
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC189255/
Abstract

Racemic 2'-deoxy-3'-thiacytidine (BCH 189) is a dideoxycytidine analog having a sulfur atom in place of the 3' carbon. The enantiomers of BCH 189 have been resolved and found to be equipotent in antiviral activity against human immunodeficiency virus types 1 and 2. However, the (-)-enantiomer (3TC) is considerably less cytotoxic than the (+)-enantiomer.

摘要

消旋2'-脱氧-3'-硫代胞苷（BCH 189）是一种双脱氧胞苷类似物，其中3'位碳原子被硫原子取代。BCH 189的对映体已被拆分，发现它们对1型和2型人类免疫缺陷病毒具有同等的抗病毒活性。然而，（-）-对映体（3TC）的细胞毒性明显低于（+）-对映体。

相似文献

1
The separated enantiomers of 2'-deoxy-3'-thiacytidine (BCH 189) both inhibit human immunodeficiency virus replication in vitro.2'-脱氧-3'-硫代胞苷（BCH 189）的分离对映体在体外均能抑制人类免疫缺陷病毒的复制。
Antimicrob Agents Chemother. 1992 Jan;36(1):202-5. doi: 10.1128/AAC.36.1.202.
2
Anti-human immunodeficiency virus type 1 activity and in vitro toxicity of 2'-deoxy-3'-thiacytidine (BCH-189), a novel heterocyclic nucleoside analog.新型杂环核苷类似物2'-脱氧-3'-硫代胞苷（BCH-189）的抗1型人类免疫缺陷病毒活性及体外毒性
Antimicrob Agents Chemother. 1991 Jul;35(7):1386-90. doi: 10.1128/AAC.35.7.1386.
3
(-)-2'-deoxy-3'-thiacytidine is a potent, highly selective inhibitor of human immunodeficiency virus type 1 and type 2 replication in vitro.（-）-2'-脱氧-3'-硫代胞苷是一种在体外对1型和2型人类免疫缺陷病毒复制具有强效、高度选择性的抑制剂。
Antimicrob Agents Chemother. 1992 Apr;36(4):733-9. doi: 10.1128/AAC.36.4.733.
4
Selective inhibition of human immunodeficiency viruses by racemates and enantiomers of cis-5-fluoro-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine.顺式-5-氟-1-[2-(羟甲基)-1,3-氧硫杂环戊烷-5-基]胞嘧啶的外消旋体和对映体对人类免疫缺陷病毒的选择性抑制作用
Antimicrob Agents Chemother. 1992 Nov;36(11):2423-31. doi: 10.1128/AAC.36.11.2423.
5
Phosphatidyl-2',3'-dideoxy-3'-thiacytidine: synthesis and antiviral activity in hepatitis B-and HIV-1-infected cells.2',3'-二脱氧-3'-硫代胞苷磷脂：在乙型肝炎和HIV-1感染细胞中的合成及抗病毒活性
Antiviral Res. 1995 Oct;28(2):113-20. doi: 10.1016/0166-3542(95)00042-k.
6
Biological comparison of wild-type and zidovudine-resistant isolates of human immunodeficiency virus type 1 from the same subjects: susceptibility and resistance to other drugs.来自同一受试者的1型人类免疫缺陷病毒野生型和齐多夫定耐药株的生物学比较：对其他药物的敏感性和耐药性
Antimicrob Agents Chemother. 1991 May;35(5):988-91. doi: 10.1128/AAC.35.5.988.
7
Activities of the four optical isomers of 2',3'-dideoxy-3'-thiacytidine (BCH-189) against human immunodeficiency virus type 1 in human lymphocytes.2',3'-二脱氧-3'-硫代胞苷（BCH-189）的四种光学异构体在人淋巴细胞中对1型人类免疫缺陷病毒的活性。
Antimicrob Agents Chemother. 1992 Mar;36(3):672-6. doi: 10.1128/AAC.36.3.672.
8
High-level resistance to (-) enantiomeric 2'-deoxy-3'-thiacytidine in vitro is due to one amino acid substitution in the catalytic site of human immunodeficiency virus type 1 reverse transcriptase.对（-）对映体2'-脱氧-3'-硫代胞苷的高水平体外抗性是由于1型人类免疫缺陷病毒逆转录酶催化位点的一个氨基酸取代。
Antimicrob Agents Chemother. 1993 Oct;37(10):2231-4. doi: 10.1128/AAC.37.10.2231.
9
Generation of drug-resistant variants of human immunodeficiency virus type 1 by in vitro passage in increasing concentrations of 2',3'-dideoxycytidine and 2',3'-dideoxy-3'-thiacytidine.通过在浓度递增的2'，3'-二脱氧胞苷和2'，3'-二脱氧-3'-硫代胞苷中进行体外传代培养，产生1型人类免疫缺陷病毒的耐药变体。
Antimicrob Agents Chemother. 1993 Jan;37(1):130-3. doi: 10.1128/AAC.37.1.130.
10
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.

引用本文的文献

1
Treatment Management Challenges in Naïve and Experienced HIV-1-Infected Individuals Carrying the M184V Mutation.初治和经治 HIV-1 感染者携带 M184V 突变的治疗管理挑战。
Viruses. 2024 Aug 30;16(9):1392. doi: 10.3390/v16091392.
2
Steady-state pharmacokinetics of lamivudine in end-stage kidney failure persons with detectable and undetectable HIV-1 RNA in peritoneal dialysis effluent.终末期肾衰竭腹膜透析患者中可检测和不可检测 HIV-1 RNA 时拉米夫定的稳态药代动力学。
Eur J Med Res. 2024 Jul 18;29(1):374. doi: 10.1186/s40001-024-01972-8.
3
Antiviral Chemotherapy in Avian Medicine-A Review.禽医学中的抗病毒化疗——综述
Viruses. 2024 Apr 12;16(4):593. doi: 10.3390/v16040593.
4
Advances in Therapeutic -Nucleosides and -Nucleic Acids with Unusual Handedness.手性治疗性核苷和核酸的研究进展。
Genes (Basel). 2021 Dec 24;13(1):46. doi: 10.3390/genes13010046.
5
Synthetic strategies toward 1,3-oxathiolane nucleoside analogues.1,3-氧硫杂环戊烷核苷类似物的合成策略。
Beilstein J Org Chem. 2021 Nov 4;17:2680-2715. doi: 10.3762/bjoc.17.182. eCollection 2021.
6
HBV/HIV Coinfection: Impact on the Development and Clinical Treatment of Liver Diseases.乙肝病毒/艾滋病毒合并感染：对肝脏疾病发展及临床治疗的影响
Front Med (Lausanne). 2021 Oct 4;8:713981. doi: 10.3389/fmed.2021.713981. eCollection 2021.
7
Putative Repurposing of Lamivudine, a Nucleoside/Nucleotide Analogue and Antiretroviral to Improve the Outcome of Cancer and COVID-19 Patients.核苷/核苷酸类似物及抗逆转录病毒药物拉米夫定的潜在新用途：改善癌症和新冠肺炎患者的治疗效果
Front Oncol. 2021 Jul 21;11:664794. doi: 10.3389/fonc.2021.664794. eCollection 2021.
8
Structural insights into the recognition of nucleoside reverse transcriptase inhibitors by HIV-1 reverse transcriptase: First crystal structures with reverse transcriptase and the active triphosphate forms of lamivudine and emtricitabine.HIV-1 逆转录酶识别核苷逆转录酶抑制剂的结构研究：与逆转录酶及拉米夫定和恩曲他滨的活性三磷酸形式的首个晶体结构。
Protein Sci. 2019 Sep;28(9):1664-1675. doi: 10.1002/pro.3681. Epub 2019 Aug 6.
9
Twenty-Five Years of Lamivudine: Current and Future Use for the Treatment of HIV-1 Infection.拉米夫定 25 年：目前和未来用于治疗 HIV-1 感染。
J Acquir Immune Defic Syndr. 2018 Jun 1;78(2):125-135. doi: 10.1097/QAI.0000000000001660.
10
Discovery and Development of the Anti-Human Immunodeficiency Virus Drug, Emtricitabine (Emtriva, FTC).发现与研制抗人类免疫缺陷病毒药物恩曲他滨（恩曲他滨，FTC）。
Acc Chem Res. 2016;49(10):2091-2098. doi: 10.1021/acs.accounts.6b00274. Epub 2016 Oct 5.

本文引用的文献

1
Frequent detection and isolation of cytopathic retroviruses (HTLV-III) from patients with AIDS and at risk for AIDS.从艾滋病患者和有患艾滋病风险的人群中频繁检测和分离出细胞病变逆转录病毒（HTLV-III）。
Science. 1984 May 4;224(4648):500-3. doi: 10.1126/science.6200936.
2
Isolation of a T-lymphotropic retrovirus from a patient at risk for acquired immune deficiency syndrome (AIDS).从一名有获得性免疫缺陷综合征（艾滋病）风险的患者体内分离出一种嗜T淋巴细胞逆转录病毒。
Science. 1983 May 20;220(4599):868-71. doi: 10.1126/science.6189183.
3
The toxicity of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. A double-blind, placebo-controlled trial.齐多夫定（AZT）治疗艾滋病及艾滋病相关综合征患者的毒性。一项双盲、安慰剂对照试验。
N Engl J Med. 1987 Jul 23;317(4):192-7. doi: 10.1056/NEJM198707233170402.
4
Resolution of racemic carbocyclic analogues of purine nucleosides through the action of adenosine deaminase. Antiviral activity of the carbocyclic 2'-deoxyguanosine enantiomers.
J Med Chem. 1987 Apr;30(4):746-9. doi: 10.1021/jm00387a032.
5
Inhibition of the in vitro infectivity and cytopathic effect of human T-lymphotrophic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV) by 2',3'-dideoxynucleosides.2',3'-双脱氧核苷对人III型嗜T淋巴细胞病毒/淋巴结病相关病毒（HTLV-III/LAV）体外感染性及细胞病变效应的抑制作用
Proc Natl Acad Sci U S A. 1986 Mar;83(6):1911-5. doi: 10.1073/pnas.83.6.1911.
6
Phase I studies of 2',3'-dideoxycytidine in severe human immunodeficiency virus infection as a single agent and alternating with zidovudine (AZT).2',3'-二脱氧胞苷作为单一药物及与齐多夫定（AZT）交替使用治疗严重人类免疫缺陷病毒感染的I期研究。
Lancet. 1988 Jan 16;1(8577):76-81. doi: 10.1016/s0140-6736(88)90283-8.
7
Sensitive and rapid assay on MT-4 cells for detection of antiviral compounds against the AIDS virus.在MT-4细胞上进行灵敏且快速的检测，以检测抗艾滋病病毒的抗病毒化合物。
J Virol Methods. 1987 Jun;16(3):171-85. doi: 10.1016/0166-0934(87)90002-4.
8
Circulating p24 antigen levels and responses to dideoxycytidine in human immunodeficiency virus (HIV) infections. A phase I and II study.
Ann Intern Med. 1989 Feb 1;110(3):189-94. doi: 10.7326/0003-4819-110-3-189.
9
Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds.用于检测抗HIV化合物的基于四氮唑的快速自动化比色测定法。
J Virol Methods. 1988 Aug;20(4):309-21. doi: 10.1016/0166-0934(88)90134-6.
10
3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro.3'-叠氮-3'-脱氧胸苷（BW A509U）：一种抗病毒剂，在体外可抑制人类III型嗜T淋巴细胞病毒/淋巴结病相关病毒的感染性和细胞病变效应。
Proc Natl Acad Sci U S A. 1985 Oct;82(20):7096-100. doi: 10.1073/pnas.82.20.7096.