Cargando…
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...
Autores principales: | , , , , , , , , , |
---|---|
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 |
_version_ | 1785015617640726528 |
---|---|
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. |
format | Online Article Text |
id | pubmed-10054226 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT tangarasalia rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT faionleo rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT piveteaucatherine rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT capetfrederic rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT godelierromain rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT michelmarion rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT flipomarion rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT deprezbenoit rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT willandnicolas rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization AT villemagnebaptiste rapidandefficientaccesstonovelbioinspired3dimensionaltricyclicspirolactamsasprivilegedstructuresviameyerslactamization |