Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams As Privileged Structures Via Meyers' Lactamization

Overview

Journal Pharmaceuticals (Basel)

Publisher MDPI

Specialty Chemistry

Date 2023 Mar 29

PMID 36986512

Authors

Salia Tangara

Leo Faion

Catherine Piveteau

Frederic Capet

Romain Godelier

Marion Michel

Marion Flipo

Benoit Deprez

Nicolas Willand

Baptiste Villemagne

Affiliations

Soon will be listed here.

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 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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