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Derivatization/Functionalization of Natural Product(RMI)

天然产物衍生化/功能化(RMI)

基本信息

批准号：
7270478
负责人：
MARVIN J MILLER
金额：
$ 31.98万
依托单位：
UNIVERSITY OF NOTRE DAME
依托单位国家：
美国
项目类别：
财政年份：
2005
资助国家：
美国
起止时间：
2005-09-23 至 2008-07-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/7270478
关键词：
Acylation Address Alkenes Alkylation Amides Amines Biochemistry Biological Biological Assay Biological Factors Cell physiology Chemicals Chemistry Collaborations Collection Commercial Sources Development Diels Alder reaction Disease Drug Delivery Systems Evaluation Future Generations Germany Goals Health Hydroxyl Radical Individual Institutes Investigation Laboratories Lead Letters Libraries Methodology Methods Microbe Microbiology Modification Natural Products Chemistry Nature Nitroso Compounds Numbers One-Step dentin bonding system Pharmaceutical Preparations Phase Polyenes Principal Investigator Productivity Proteins Publishing Range Reaction Research Resources Scheme Screening procedure Solid Solutions Source Structure Testing United States National Institutes of Health adduct analog antimicrobial drug base chemical synthesis combinatorial chemistry cycloaddition design diene functional group high throughput screening hydroxamate interest method development novel programs response scaffold size small molecule solid solution

项目摘要

DESCRIPTION (provided by applicant): This proposal is being submitted in response to RFA-RM-05-013 (New Methodologies for Natural Products Chemistry). The hypothesis of this proposal is that cycloadducts and ene products derived from reactions of diene- and alkene-containing natural products with nitroso moieties, will provide novel derivatives that can serve as versatile building blocks (evolvable scaffolds) for syntheses of a number of important and often new bioactive molecules. Specific Aims Are: 1. Generate novel scaffolds from diene and alkene-containing natural products by simple one step cycloaddition and ene reactions with a variety of nitroso compounds, even those that contain extensive additional functionality. Both solution phase chemistry and novel "natural product solid phase capture" methods will be described. 2. Demonstrate that the newly functionalized natural product scaffolds are "evolvable platforms" that can be elaborated to both conformationally restricted and more flexible libraries using novel chemistry developed in the PI's laboratory and classical chemistry in the labs of the described collaborators as well as in the PI's labs. 3. Broadly test the scaffold and derived libraries of novel compounds using the extensive set of assays in place at the Hans-Knoll Institute for Natural Products Research (HKI).

描述（由申请人提供）：本提案是根据RFA-RM-05-013（天然产物化学新方法）提交的。该提议的假设是，环加合物和烯产物衍生自含二烯和烯烃的天然产物与亚硝基部分的反应，将提供新的衍生物，其可以用作合成许多重要的并且通常是新的生物活性分子的通用构建块（可进化的支架）。具体目标是：1。通过简单的一步环加成和与各种亚硝基化合物的烯反应，从二烯和含烯烃的天然产物中产生新型支架，即使是那些含有大量额外功能的化合物。溶液相化学和新的“天然产物固相捕获”方法将被描述。2.证明新功能化的天然产物支架是“可进化的平台”，可以使用PI实验室开发的新化学和所述合作者实验室以及PI实验室中的经典化学，将其加工成构象受限和更灵活的文库。3.使用Hans-Knoll天然产物研究所（HKI）的一套广泛的检测方法，广泛测试新型化合物的支架和衍生库。