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Methodology for, and Synthesis of Biologically Active Pyrrolidinone Natural Products.

生物活性吡咯烷酮天然产物的方法学和合成。

基本信息

批准号：
EP/J004499/1
负责人：
Jonathan Burton
金额：
$ 45.98万
依托单位：
University of Oxford
依托单位国家：
英国
项目类别：
Research Grant
财政年份：
2012
资助国家：
英国
起止时间：
2012 至无数据
项目状态：
已结题

来源：
https://gtr.ukri.org/projects?ref=EP%2FJ004499%2F1
关键词：
Methodology Synthesis Biologically Active Pyrrolidinone

项目摘要

Five-membered ring compounds with contain one nitrogen atom, are ubiquitous structural units present on thousands of natural products, in numerous brand-name drugs and agrochemicals, and are widely used to modify catalysts for a particular purpose. These nitrogen "heterocycles" are present in a family of highly complex natural products which exhibit antitumour and antibiotic activity. The search for new antibiotics is particularly important now we are in the "post-penicillin" era and our entering the era when even resistance to antibiotics such as vancomycin is regularly encountered. The search for new antibiotics with different modes of action is an important challenge facing academia and the pharmaceutical industry. The aim of our work is to develop new and efficient methods for the synthesis of nitrogen heterocycles which will have particular application to the synthesis of these antitumour antibiotics. A major part of the project will involve using the developed methodologies to synthesise one of the natural products and, importantly, to prepare simplified analogues. The simplified analogues will be tested for both antibiotic and antitumour activity. In the long term, this research may have an impact on the discovery of new antibiotics and antitumour agents. Moreover, the developed methodologies will have application in the synthesis of a whole range of other biologically important natural products and small molecules.

五元环化合物含有一个氮原子，是存在于数千种天然产品、众多名牌药物和农用化学品中的普遍结构单元，被广泛用于为特定目的而修饰催化剂。这些氮“杂环”存在于一类高度复杂的天然产物中，这些天然产物具有抗肿瘤和抗菌活性。现在我们正处于“后青霉素”时代，进入了一个甚至经常遇到万古霉素等抗生素耐药性的时代，寻找新的抗生素尤为重要。寻找具有不同作用模式的新抗生素是学术界和制药行业面临的重要挑战。我们工作的目的是开发新的高效的氮杂环化合物的合成方法，这将在这些抗肿瘤抗生素的合成中具有特殊的应用。该项目的一个主要部分将涉及使用开发的方法来合成一种天然产品，更重要的是，制备简化的类似物。简化的类似物将同时进行抗生素和抗肿瘤活性测试。从长远来看，这项研究可能会对发现新的抗生素和抗肿瘤药物产生影响。此外，所开发的方法将应用于合成一系列其他具有生物重要性的天然产物和小分子。