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Keywords = tricyclic spirolactams

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26 pages, 21117 KiB  
Article
Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization
by Salia Tangara, Léo Faïon, Catherine Piveteau, Frédéric Capet, Romain Godelier, Marion Michel, Marion Flipo, Benoit Deprez, Nicolas Willand and Baptiste Villemagne
Pharmaceuticals 2023, 16(3), 413; https://doi.org/10.3390/ph16030413 - 8 Mar 2023
Cited by 1 | Viewed by 3058
Abstract
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 [...] Read more.
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. Full article
(This article belongs to the Special Issue Privileged Structures as Leads in Medicinal Chemistry 2023)
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