H2020Индивидуална стипендия2015–2017

ORGANO-GOLD CAT · Merging organo- and gold-catalysis to design cascade reactions: a shortcut toward molecular complexity

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

Период: 2015-06-01 → 2017-05-31
Финансиране от ЕС: 158 122 €
Участници: 1
Схема: MSCA-IF-EF-ST

Линиите свързват координатора с партньорите.

Накратко на български

Комбинирането на органичен и златен катализатори цели създаването на сложни молекули, подобни на тези в природата, само в една стъпка. Това помага за по-ефективното откриване на нови структури, които могат да станат основа за бъдещи 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

Merging organo- and gold-catalysis to design cascade reactions: a shortcut toward molecular complexity

We are in a changing era for drug discovery: the growing perception is that basic chemical research will play a greater role in pharmaceutical development. One current challenge is to develop a new kind of chemistry that yields a screening collection comprising optimal chiral molecules that increase the probability of success in identifying drug-candidate structures. The proposed research aims to develop conceptually innovative catalytic methods to rapidly generate, in one single step, architecturally complex chiral natural-like compounds. Natural products have been selected in evolution and their underlying structural scaffolds define biologically relevant fractions of chemical space. Consequently, compound libraries inspired by natural structures deliver lead candidates with a higher hit-rate than conventional lead generation strategies. More specifically, the goal of the research project is to combine the potential of asymmetric organocatalysis and gold catalysis, powerful fields of molecule activation, to find cost-effective synthetic methods for reproducing the rich structural diversity of natural molecules. The resulting synthetic library constitutes an ideal starting point for biological screening carried out in collaboration with a world-wide recognized pharma-company (Lundbeck A/S), will increase the probability of success in identifying drug-candidat estructures. The development of the proposed research encoutered a very moderate succes, and the combination of two distinct catalytic cycles proved much more challenging than expected. As a consequence, it has been impossible to access the targeted library of complex molecules in an enantiopure form, as requiered for biological screening, menaing the impossibility of conducing test and lead optimisations as initially planned with Lundbeck A/S, our industrial partner.

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

Цел на проекта

We are in a changing era for drug discovery: the growing perception is that basic chemical research will play a greater role in pharmaceutical development. One current challenge is to develop a new kind of chemistry that yields a screening collection comprising optimal chiral molecules that increase the probability of success in identifying drug-candidate structures. The proposed research aims to develop conceptually innovative catalytic methods to rapidly generate, in one single step, architecturally complex chiral natural-like compounds. Natural products have been selected in evolution and their underlying structural scaffolds define biologically relevant fractions of chemical space. Consequently, compound libraries inspired by natural structures deliver lead candidates with a higher hit-rate than conventional lead generation strategies.We will pursue the proposed research project under the guiding principle that compound development should be driven by discoveries and innovation in chemical methodology. The goal of the research project is to combine the potential of asymmetric organocatalysis and gold catalysis, powerful fields of molecule activation, to find cost-effective synthetic methods for reproducing the rich structural diversity of natural molecules. Since the vast majority of natural products and drug-like compounds possess heterocyclic moieties, we will focus on preparing diverse heterocyclic compounds, especially based on the furan unit. The resulting synthetic platform will be used as an ideal starting point for assembling enantiopure chiral 2,3-furan fused carbocycles, which, along with biological screening carried out in collaboration with a world-wide recognized pharma-company (Lundbeck A/S), will increase the probability of success in identifying drug-candidate structures. The multi-cultural nature of this project will greatly contribute to broaden the fellow competencies and will place him in an excellent position for the next career move

Оригинален текст от CORDIS (на английски).

Участници

FUNDACIO INSTITUT CATALA D'INVESTIGACIO QUIMICA · TARRAGONAКоординаторИспания