Overseas Travel Grant: From Dendralenes to Antimicrobial Decalins (Visit to Research School of Chemistry, Australian National University)

海外旅费资助：从Dendralenes到抗菌十氢萘（参观澳大利亚国立大学化学研究院）

基本信息

批准号：
EP/R024758/1
负责人：
Paul Clarke
金额：
$ 1.49万
依托单位：
University of York
依托单位国家：
英国
项目类别：
Research Grant
财政年份：
2017
资助国家：
英国
起止时间：
2017 至无数据
项目状态：
已结题

来源：
https://gtr.ukri.org/projects?ref=EP%2FR024758%2F1
关键词：
Overseas Travel Grant Dendralenes Antimicrobial

项目摘要

Bacterial infections are becoming increasingly hard to treat with current antibiotics and it is well recognised that new treatments are required. The government and the WHO continue to highlight the development of new antibiotics as an area of high priority. Many antimicrobial natural products contain functionalised decalin ring systems. These structural units are synthetically non-trivial to construct and oftentimes require many synthetic steps. It is proposed here that recent advances in the synthesis and characterisation of dendralenes may enable the development of a highly efficient and general transmissive Diels-Alder approach to a large range of functionalised decalin ring systems present in many natural products. If successful, such a route could lead to breakthroughs in the synthesis and supply of these scarce molecules for full biological evaluation. This proposal will build on our previous EPSRC-funded work in the area antimicrobial natural product synthesis and the use of Diels-Alder reactions for the synthesis of biologically active natural products by allowing the PI to spend a period of time embedded in the Sherburn group to gain first-hand experience in the synthesis and handling of dendralenes. This will enable a full proposal for the use of dendralenes in the synthesis of decalin-containing antimicrobials to be developed.

细菌感染越来越难以治疗目前的抗生素治疗，人们认识到需要新的治疗方法。政府和谁继续强调新抗生素的发展是一个优先级的领域。许多抗微生物天然产品都包含功能化的脱甲酸环蛋白环系统。这些结构单元在构造上是不平凡的，通常需要许多合成步骤。这里提出的是，在室园的合成和表征的最新进展可能使高效且普遍的传播Diels-Alder方法开发到许多天然产物中存在的大量功能性的脱甲酸地带系统。如果成功，这种途径可能会导致这些稀缺分子的合成和供应进行全面生物学评估的突破。该提案将基于我们以前由EPSRC资助的抗菌天然产品合成的工作，以及使用Diels-Alder反应用于合成生物活性天然产物的综合，通过允许PI花费一段时间嵌入在Sherburn组中的一段时间，以获得在甲状腺丁氏甲状腺丁二菜的合成和操作方面的第一手经验。这将使能够在合成含脱丙酸脱丁质的抗微生物的合成中使用dendralens的完整建议。