NOVEL HIV1 SPECIFIC NON-NUCLEOSIDE RT INHIBITOR

新型 HIV1 特异性非核苷 RT 抑制剂

基本信息

  • 批准号:
    2417554
  • 负责人:
  • 金额:
    $ 10万
  • 依托单位:
  • 依托单位国家:
    美国
  • 项目类别:
  • 财政年份:
    1997
  • 资助国家:
    美国
  • 起止时间:
    1997-09-01 至 1998-02-28
  • 项目状态:
    已结题

项目摘要

This proposal is to develop a HIV-1 specific nonnucleoside RT inhibitor. This compound has been shown to have EC50 values ranging from 0.4-1.7 microM against both laboratory and clinical HIV- isolates in the in vitro XTT assay. It is also active against HIV isolates with a mutation of Y181C, against 3TC-resistant isolates with an RT mutation of M184I, and against HEPT-resistant isolates with a mutation of P236L. Furthermore, the compound exhibits potent activity against human cytomegalovirus with an EC50 value comparable to that of ganciclovir. Further pharmacological and toxicological evaluations of the drug will be the focus of this phase I SBIR program, which include synthesis of one kilogram of (+)-12- oxocalanolide A, improving the synthetic processes of (+)-12- oxocalanolide A, and performing the acute single-dose toxicity studies. The toxicity study will examine oral and intravenous administration of the inhibitor in two mammalian species, and begin preliminary pharmacokinetic experiments. The ultimate goal for this SBIR program will be to file an IND application with the FDA at the end of the Phase II SBIR and to initiate a Phase I/II clinical trial.
该建议是开发HIV-1特异性非核苷RT

项目成果

期刊论文数量(2)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI.
  • DOI:
    10.1016/s0960-894x(98)00380-1
  • 发表时间:
    1998-08
  • 期刊:
  • 影响因子:
    2.7
  • 作者:
    Z. Q. Xu;R. Buckheit;T. L. Stup;M. Flavin;A. Khilevich;J. Rizzo;L. Lin;D. Zembower
  • 通讯作者:
    Z. Q. Xu;R. Buckheit;T. L. Stup;M. Flavin;A. Khilevich;J. Rizzo;L. Lin;D. Zembower
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ZE-QI XU其他文献

ZE-QI XU的其他文献

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{{ truncateString('ZE-QI XU', 18)}}的其他基金

Nanoscale Metal-Organic Frameworks as X-ray Activatable Cancer Vaccines
纳米级金属有机框架作为 X 射线激活癌症疫苗
  • 批准号:
    10558960
  • 财政年份:
    2022
  • 资助金额:
    $ 10万
  • 项目类别:
DEVELOPMENT OF NOVEL PHARMACOPHORE WITH ANTI-TB ACTIVITY
具有抗结核活性的新型药效团的开发
  • 批准号:
    6311243
  • 财政年份:
    2001
  • 资助金额:
    $ 10万
  • 项目类别:
NOVEL PHOSPHONATE NUCLEOTIDE ANALOGS AS ANTIHIV AGENTS
作为抗艾滋病毒药物的新型膦酸酯核苷酸类似物
  • 批准号:
    2075172
  • 财政年份:
    1995
  • 资助金额:
    $ 10万
  • 项目类别:
SYNTHESIS OF NOVEL ACYCLONUCLEOTIDES AS ANTIHIV AGENTS
作为抗HIV药物的新型环核苷酸的合成
  • 批准号:
    2074063
  • 财政年份:
    1995
  • 资助金额:
    $ 10万
  • 项目类别:

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  • 批准号:
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  • 财政年份:
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  • 资助金额:
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  • 财政年份:
    1997
  • 资助金额:
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