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Issue 71, 2020
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Three cheers for nitrogen: aza-DKPs, the aza analogues of 2,5-diketopiperazines

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Abstract

Nitrogen-containing heterocycles represent a major source of pharmacological probes and drug candidates. To extend their molecular diversity and their potential biological activities, it is of importance to design and synthesize new N-heterocyclic scaffolds. Therefore, aza-diketopiperazines (aza-DKPs), the aza analogues of well-known 2,5-diketopiperazines (DKPs), emerged as a promising new scaffold. Although the first synthesis of an aza-DKP dates from 1951, significant developments have been made during the last decade. This feature article summarizes the different synthetic strategies to access and functionalise aza-DKPs. Their biological properties and potential applications in medicinal chemistry and drug discovery are discussed as well.

Graphical abstract: Three cheers for nitrogen: aza-DKPs, the aza analogues of 2,5-diketopiperazines

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Article information


Submitted
06 Nov 2020
Accepted
10 Nov 2020
First published
07 Dec 2020

This article is Open Access

RSC Adv., 2020,10, 43358-43370
Article type
Review Article

Three cheers for nitrogen: aza-DKPs, the aza analogues of 2,5-diketopiperazines

T. Maujean, N. Girard, A. Ganesan, M. Gulea and D. Bonnet, RSC Adv., 2020, 10, 43358
DOI: 10.1039/D0RA09457A

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