Issue 5, 2022

Recent developments in the utility of saturated azaheterocycles in peptidomimetics

Abstract

To a large extent, the physical and chemical properties of peptidomimetic molecules are dictated by the integrated heterocyclic scaffolds they contain. Heterocyclic moieties are introduced into a majority of peptide-mimicking molecules to modulate conformational flexibility, improve bioavailability, and fine-tune electronics, and in order to achieve potency similar to or better than that of the natural peptide ligand. This mini-review delineates recent developments, limited to the past five years, in the utility of selected saturated 3- to 6-membered heterocyclic moieties in peptidomimetic design. Also discussed is the chemistry involved in the synthesis of the azaheterocyclic scaffolds and the structural implications of the introduction of these azaheterocycles in peptide backbones as well as side chains of the peptide mimics.

Graphical abstract: Recent developments in the utility of saturated azaheterocycles in peptidomimetics

Article information

Article type
Review Article
Submitted
08 juil. 2021
Accepted
22 déc. 2021
First published
24 déc. 2021

Org. Biomol. Chem., 2022,20, 963-979

Recent developments in the utility of saturated azaheterocycles in peptidomimetics

M. K. Singh and M. K. Lakshman, Org. Biomol. Chem., 2022, 20, 963 DOI: 10.1039/D1OB01329G

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