POLYKETOMACROCYCLES · Transannular Macrocyclisation and the concise total synthesis of Antifungal natural products
6РП — Действия „Мария Кюри“
- Период
- 2005-11-01 → 2007-07-31
- Финансиране от ЕС
- 158 479 €
- Участници
- 1
- Схема
- EIF
Линиите свързват координатора с партньорите. За проекти отпреди 2014 г. CORDIS не винаги дава точни координати. Тези точки са на ниво град или държава.
Накратко на български
Синтезирането на природни съединения като зеараленон и 15G256b се извършва чрез нови химични методи за създаване на големи пръстенови структури. Това помага за изследване на противогъбичните свойства на тези вещества и връзката между тяхната структура и биологичното им действие.
Кратко обяснение, генерирано от езиков модел по текста на CORDIS. Оригиналът е по-долу.
Цел на проекта
The Barrett group has carried out extensive research on the synthesis of antifungal natural products and the underlying synthetic methodology with recent focus on targets such as nikkomycin B, papuamine, papulacandin, FR-900848, pramanicin, the palmarumyci ns and preussomerin G.This proposal concerns the total synthesis of two bioactive natural products zearalenone and 15G256b. These two macrocyclic compounds are respectively a mycotoxin and an antifungal agent. They possess a highly functionalised macrocycl ic core and 2,4-dihydroxybenzoic acid units, which are constituents of numerous macrocyclic bioactive natural products.The first objective of the research is the development of new and original strategies, which should allow concise access to these natural compounds. The first key step is the macrocyclisation reaction, which takes place by using an unusual metathesis reaction between an alkene and an alkyne, following an approach recently developed at Imperial College London. The second key step involves a transannular reaction to elaborate the arene entity fused to the macrocyclic ring by a biomimetic closure of triketo-ester moiety. The second objective of this work is the biological testing of the synthesised compounds by GlaxoSmithKline in the United Kingdom to evaluate their activities.This proposal describes a programme of interdisciplinary research. First, it is a synthetic chemistry because these polyfunctionalised compounds will be prepared by using original strategies and new methodologies. Secondly, it is also a medicinal chemistry because this route to zearalenone and 15G256b is also promising in that it could be applicable to others members of these classes of natural products and also allowing for the determination of structure-activity relationship with the antifungal agent 15G256b. The new synthetic methods should be of general interest for the preparation of diverse complex aromatic compounds of pharmaceutical importance.
Оригинален текст от CORDIS (на английски).
Участници
- IMPERIAL COLLEGE LONDON, DEPARTMENT OF CHEMISTRY · LONDONКоординаторНиво градОбединеното кралство
Връзки
Данни: CORDIS, © Европейски съюз