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Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization

The concept of privileged structure has been used as a fruitful approach for the discovery of novel biologically active molecules. A privileged structure is defined as a semi-rigid scaffold able to display substituents in multiple spatial directions and capable of providing potent and selective liga...

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Autores principales: Tangara, Salia, Faïon, Léo, Piveteau, Catherine, Capet, Frédéric, Godelier, Romain, Michel, Marion, Flipo, Marion, Deprez, Benoit, Willand, Nicolas, Villemagne, Baptiste
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10054226/
https://www.ncbi.nlm.nih.gov/pubmed/36986512
http://dx.doi.org/10.3390/ph16030413
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author Tangara, Salia
Faïon, Léo
Piveteau, Catherine
Capet, Frédéric
Godelier, Romain
Michel, Marion
Flipo, Marion
Deprez, Benoit
Willand, Nicolas
Villemagne, Baptiste
author_facet Tangara, Salia
Faïon, Léo
Piveteau, Catherine
Capet, Frédéric
Godelier, Romain
Michel, Marion
Flipo, Marion
Deprez, Benoit
Willand, Nicolas
Villemagne, Baptiste
author_sort Tangara, Salia
collection PubMed
description The concept of privileged structure has been used as a fruitful approach for the discovery of novel biologically active molecules. A privileged structure is defined as a semi-rigid scaffold able to display substituents in multiple spatial directions and capable of providing potent and selective ligands for different biological targets through the modification of those substituents. On average, these backbones tend to exhibit improved drug-like properties and therefore represent attractive starting points for hit-to-lead optimization programs. This article promotes the rapid, reliable, and efficient synthesis of novel, highly 3-dimensional, and easily functionalized bio-inspired tricyclic spirolactams, as well as an analysis of their drug-like properties.
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spelling pubmed-100542262023-03-30 Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization Tangara, Salia Faïon, Léo Piveteau, Catherine Capet, Frédéric Godelier, Romain Michel, Marion Flipo, Marion Deprez, Benoit Willand, Nicolas Villemagne, Baptiste Pharmaceuticals (Basel) Article The concept of privileged structure has been used as a fruitful approach for the discovery of novel biologically active molecules. A privileged structure is defined as a semi-rigid scaffold able to display substituents in multiple spatial directions and capable of providing potent and selective ligands for different biological targets through the modification of those substituents. On average, these backbones tend to exhibit improved drug-like properties and therefore represent attractive starting points for hit-to-lead optimization programs. This article promotes the rapid, reliable, and efficient synthesis of novel, highly 3-dimensional, and easily functionalized bio-inspired tricyclic spirolactams, as well as an analysis of their drug-like properties. MDPI 2023-03-08 /pmc/articles/PMC10054226/ /pubmed/36986512 http://dx.doi.org/10.3390/ph16030413 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tangara, Salia
Faïon, Léo
Piveteau, Catherine
Capet, Frédéric
Godelier, Romain
Michel, Marion
Flipo, Marion
Deprez, Benoit
Willand, Nicolas
Villemagne, Baptiste
Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization
title Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization
title_full Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization
title_fullStr Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization
title_full_unstemmed Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization
title_short Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization
title_sort rapid and efficient access to novel bio-inspired 3-dimensional tricyclic spirolactams as privileged structures via meyers’ lactamization
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10054226/
https://www.ncbi.nlm.nih.gov/pubmed/36986512
http://dx.doi.org/10.3390/ph16030413
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