H2020Индивидуална стипендия2016–2018

SYNOX · Total Synthesis of Biologically Important Pyrrolidinone Natural Products and Analogues Thereof.

„Хоризонт 2020“ — Действия „Мария Склодовска-Кюри“

Период
2016-09-01 → 2018-08-31
Финансиране от ЕС
183 455 €
Участници
1
Схема
MSCA-IF-EF-ST

Линиите свързват координатора с партньорите.

Накратко на български

Синтезирането на природни съединения като интомицините и оксазоломицините се извършва чрез по-екологични химични методи. Това помага за по-доброто разбиране на техните антибактериални, противотуморни и противовирусни свойства с цел бъдещо разработване на нови лекарства.

Този кратък обзор е генериран от изкуствен интелект

Кратко обяснение, генерирано от езиков модел по текста на CORDIS. Оригиналът е по-долу.

Резултати накратко

Total Synthesis of Biologically Important Pyrrolidinone Natural Products and Analogues Thereof.

Natural products are the active components of many traditional medicines. A large number of currently prescribed drugs are either directly derived from or inspired by natural products. However, the availability of natural products from natural sources can be limited mkaing the full study their properties very challenging. Hence, there is always a need for greener, economic synthetic methodologies for the synthesis of natural products and analogues for the better understanding of their bioactivities with the future prospect of developing novel drugs. Considering the huge importance of natural products in drug discovery, in the proposal, we developed the synthesis of all three members of Inthomycins and C-16 substituted core of the oxazolomycins. These natural products display a wide variety of biological properties, including antibiotic activity, anti-tumour activity and anti-viral activity, thus developing a route has the potential for to benefitfor society in the future. Apart from this, our strategy offers an advancement over the previous literature in terms of sustainability and environment-friendly chemical process that avoids the use of highly toxic chemicals as well as potentially hazardous materials. The synthesis of the inthomycins has been executed from simple and readily available starting materials to obtain the final core of these natural products efficiently, and should allow the futuer synthesis of the further biologically active natural products the oxazolomycins. The work conducted during the fellowship will facilitate Dr Kumar to obtain an independent academic research position because during these 2 years he has been able to develop and widen his competences, particularly in terms of multi/interdisciplinary and inter-sectoral experience and transferable skills. The novel strategies and reactions developed during this fellowship will advance the field of total synthesis of complex biologically active natural products and natural products fragments, which will be useful for both academic and pharmaceutical industries. In addition, the avoidance of toxic material is an advancement to the previous work and a further step towards the environmentally friendly protocols. Also, these natural products have already shown wide range of biological activities. Thus, the developed synthetic strategies will contribute to the social and economic benefit in the Horizon 2020 Programme. Furthermore, the research carried out during the tenure of this fellowship has definitely enhanced the innovation capacity, and helped the candidate develop these critical skills, which are valuable for his career. The work conducted during these two years of fellowship has been published in a high-ranked journal and one more document will be forthcoming published. Also, work has been presented at many places including academic meetings and industrial symposiums, in which a high interest has been shown from other researchers.

Текст от CORDIS, на английски · Данни: CORDIS, © Европейски съюз

Цел на проекта

The importance of natural products and derivatives as sources of new drugs is undeniable. Newman has stated: ""It is probably true that if one had to name the natural product that has saved the most lives.....penicillin G would be the molecule of choice"" (D. J. Newman, G. M. Cragg, in Natural Product Chemistry for Drug Discovery, Chapter 1, RSC Biolmolecular Sciences No. 18, 2009). In this proposal we will develop methodology for the synthesis of two types of closely related natural products which have wide-ranging biological activities including: anti-bacterial, anti-viral, anti-tumour and herbicidal activity; but whose biological activities have not been fully evaluated. We will use our recently developed oxidative radical cyclisation methodology to synthesise the cores of these biologically relevant natural products and develop new methodology for the direct functionalisation of certain aromatic heterocycles as part of the synthesis of the unsaturated portions of the natural products. The biological activities, particularly with respect to anti-bacterial and anti-tumour properties of all of the key synthetic intermediates (simplified analogues) and synthetic natural products themselves will be assessed.The project is divided into four work packages involving: i) development of direct functionalisation certain aromatic heterocycles; ii) synthesis of the the one type of natural product; iii) oxidative radical synthesis of natural product cores; iv) total synthesis of the second type of natural product.""

Оригинален текст от CORDIS (на английски).

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Данни: CORDIS, © Европейски съюз