A PRACTICAL SYNTHETIC ROUTE TO THE TETRACYCLINES
四环素类药物的实用合成路线
基本信息
- 批准号:6835644
- 负责人:
- 金额:$ 32.83万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2001
- 资助国家:美国
- 起止时间:2001-01-01 至 2005-12-31
- 项目状态:已结题
- 来源:
- 关键词:Diels Alder reactionantibioticsantineoplastic antibioticsbenzoatesbenzofuranschemical additionchemical structure functioncombinatorial chemistrycyclohexanonesdrug design /synthesis /productiondrug resistanceintermolecular interactionmolecular shapep aminobenzoatepalladiumstereochemistrystereoisomertetracyclines
项目摘要
DESCRIPTION: (Principal Investigator's Abstract) The objective of this proposal
is to develop the first practical, efficient, and enantioselective laboratory
synthetic route(s) to the tetracycline antibiotics. The goal is to devise a
route of twelve or fewer synthetic steps, perhaps as few as eight steps,
beginning with benzoic acid as a starting material. A constraint that the
synthetic route be versatile is also imposed, allowing for the introduction of
substantive structural variability at a late stage, particularly within the C
and D rings of the tetracycline structure, where prior research has shown that
there is great opportunity for antibiotic development. Synthesis of a wide
range of new tetracyclines for evaluation as improved antibiotics and,
potentially antitumor agents is proposed. A particular focus is the development
of effective antibiotics against tetracycline-resistant microorganisms.
Adaptation and/or modification of these synthetic routes to target new
tetracycline structures with antitumor activity, such as SF-2575 (TAN-1518 X)
will also be attempted.
描述:(主要研究者摘要)本提案的目的
是建立第一个实用、高效和对映选择性的实验室,
四环素类抗生素的合成途径。我们的目标是设计一个
合成路线为12步或更少的合成步骤,可能少至8步,
以苯甲酸作为起始原料开始。一个约束,
合成路线也是通用的,允许引入
后期阶段的实质性结构变化,特别是在C
和四环素结构的D环,先前的研究表明,
抗生素的发展有很大的机会。合成一个广泛的
一系列新的四环素类抗生素作为改进的抗生素进行评价,
提出了潜在的抗肿瘤剂。一个特别的重点是发展
针对四环素耐药微生物的有效抗生素。
调整和/或修饰这些合成路线以靶向新的
具有抗肿瘤活性的四环素结构,如SF-2575(TAN-1518 X)
也将尝试。
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
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ANDREW G MYERS其他文献
ANDREW G MYERS的其他文献
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{{ truncateString('ANDREW G MYERS', 18)}}的其他基金
Discovery through chemical synthesis of antibiotics effective against modern bacterial pathogens
通过化学合成发现对现代细菌病原体有效的抗生素
- 批准号:
10570180 - 财政年份:2022
- 资助金额:
$ 32.83万 - 项目类别:
Discovery through chemical synthesis of antibiotics effective against modern bacterial pathogens
通过化学合成发现对现代细菌病原体有效的抗生素
- 批准号:
10419458 - 财政年份:2022
- 资助金额:
$ 32.83万 - 项目类别:
A PRACTICAL SYNTHETIC ROUTE TO THE TETRACYCLINES
四环素类药物的实用合成路线
- 批准号:
6626402 - 财政年份:2001
- 资助金额:
$ 32.83万 - 项目类别:
A PRACTICAL SYNTHETIC ROUTE TO THE TETRACYCLINES
四环素类药物的实用合成路线
- 批准号:
6893948 - 财政年份:2001
- 资助金额:
$ 32.83万 - 项目类别:
A PRACTICAL SYNTHETIC ROUTE TO THE TETRACYCLINES
四环素类药物的实用合成路线
- 批准号:
6692976 - 财政年份:2001
- 资助金额:
$ 32.83万 - 项目类别:
A PRACTICAL SYNTHETIC ROUTE TO THE TETRACYCLINES
四环素类药物的实用合成路线
- 批准号:
6488779 - 财政年份:2001
- 资助金额:
$ 32.83万 - 项目类别:
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