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Enantioselective strategies for the synthesis of phenyl bioisosteres

Project description

Advancing enantioselective synthesis for drug discovery

In drug discovery, enantioenriched molecules are crucial, as even slight differences between enantiomers can lead to vastly different biological effects. However, obtaining these molecules can be challenging. Traditional approaches often rely on aromatic rings, which are two-dimensional and can limit chemical diversity. To overcome this, the medicinal chemistry field is turning to saturated scaffolds, offering greater three-dimensionality and access to novel chemical spaces. Supported by the Marie Skłodowska-Curie Actions programme, the EnantioBioIso project aims to revolutionise this area by developing new enantioselective strategies for synthesising phenyl bioisosteres. These strategies will unlock the potential of polycyclic bridged skeletons, offering exciting new pathways for drug discovery and advancing medicinal chemistry.

Objective

The obtainment of enantioenriched molecules is of fundamental importance since two enantiomers of the same drug candidate can display completely different biological properties. In recent years, an increasing interest in employing saturated scaffolds has been observed in medicinal chemistry since they provide tridimensionality and well-defined exit vectors that give access to novel unexplored chemical space, leading to a higher success in drug discovery programs. Among them, some polycyclic bridged skeletons have been identified as suitable saturated bioisosteres of aromatic rings which represent the common two-dimensional, flat moieties that are routinely employed in the drug discovery process. The aim of EnantioBioIso is to provide novel enantioselective strategies for the synthesis of phenyl bioisosteres, enabling unprecedented approaches to obtain bridged skeletons that are of fundamental importance for medicinal chemistry.

Fields of science (EuroSciVoc)

Keywords

Programme(s)

Topic(s)

Funding Scheme

HORIZON-TMA-MSCA-PF-EF - HORIZON TMA MSCA Postdoctoral Fellowships - European Fellowships

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Call for proposal

(opens in new window) HORIZON-MSCA-2023-PF-01

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Coordinator

UNIVERSIDAD AUTONOMA DE MADRID
Net EU contribution
€ 165 312,96
Address
CALLE EINSTEIN 3 CIUDAD UNIV CANTOBLANCO RECTORADO
28049 Madrid
Spain
Region
Comunidad de Madrid Comunidad de Madrid Madrid
Activity type
Higher or Secondary Education Establishments
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Total cost
No data

Partners (1)