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DIDEOXYNUCLEOSIDES AS POTENTIAL ANTI-AIDS DRUGS

DIDEOXYNUCLEOSIDES AS POTENTIAL ANTI-AIDS DRUGS
双脱氧核苷作为潜在的抗艾滋病药物
批准号：
3838034
负责人：
V E MARQUEZ
金额：
$0.0万
依托单位：
DIVISION OF CANCER TREATMENT
依托单位国家：
美国
项目类别：
财政年份：
--
资助国家：
美国
项目状态：
未结题
起止时间：
至
来源：
https://reporter.nih.gov/project-details/3838034
关键词：
2'3' dideoxynucleoside adenosine deaminase antiAIDS agent antiviral agents chemical structure function conformation cyclic compound drug design /synthesis /production human immunodeficiency virus nuclear magnetic resonance spectroscopy prodrugs purine analog

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中文摘要
翻译
一系列新的糖基修饰2‘，3’-二脱氧-2‘，3’-二氟核苷 并测定了它们的核磁共振溶液构象。 特定形式的环状褶皱与抗艾滋病毒活性相关。 几种新型的发酵扩环碳环类似物 合成产物oxetanocin A并对其抗HIV活性进行评价 活动。与双脱氧核糖相反，这些化合物 缺乏抗艾滋病病毒的活性。 选择酸性稳定的6-X-取代-(2‘-氟-2’， 3‘-dideoxy-beta-D-threo-pentofuranosyl)purines(X=F，Cl，Br，I，NHMe， Nhet、NHOH、NHOMe、NHOCH2 Ph)作为抗HIV腺苷 脱氨酶激活的“前药物”。他们的评估正在进行中。
英文摘要
A series of new sugar-modified 2',3'-dideoxy-2',3'-difluoro nucleosides were synthesized and the NMR solution conformations were determined. Specific forms of ring puckering were correlated with anti-HIV activity. A number of novel ring-expanded carbocyclic analogues of the fermentation product oxetanocin A were synthesized and evaluated for anti-HIV activity. As opposed to the dideoxyribose counterparts, these compounds were devoid of anti-HIV activity. Selected acid-stable 6-X-substituted-(2'-fluoro-2', 3'-dideoxy-beta-D-threo-pentofuranosyl)purines (X = F, Cl, Br, I, NHMe, NHEt, NHOH, NHOMe, NHOCH2 Ph) were prepared as anti-HIV adenosine deaminase-activated "pro-drugs". Their evaluation is in progress.
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ENZYME INHIBITORS AS PROTENTIAL ANTICANCER AND ANTIVIRAL DRUGS
  • 批准号：
    5201243
  • 项目类别：
  • 资助金额：
    $0.0万
  • 财政年份：
    --
  • 负责人：
    V E MARQUEZ
  • 依托单位：
    DIVISION OF CANCER TREATMENT
DIDEOXYNUCLEOSIDES AS POTENTIAL ANTI-AIDS DRUGS
  • 批准号：
    5201241
  • 项目类别：
  • 资助金额：
    $0.0万
  • 财政年份：
    --
  • 负责人：
    V E MARQUEZ
  • 依托单位：
    DIVISION OF CANCER TREATMENT
CYCLOPENTENYL NUCLEOSIDE ISOSTERES AS POTENTIAL ANTITUMOR AND ANTIVIRAL AGENTS
  • 批准号：
    5201242
  • 项目类别：
  • 资助金额：
    $0.0万
  • 财政年份：
    --
  • 负责人：
    V E MARQUEZ
  • 依托单位：
    DIVISION OF CANCER TREATMENT
DIDEOXYNUCLEOSIDES AS POTENTIAL ANTI-AIDS DRUGS
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