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

Maujean, Timothé, Girard, Nicolas, Ganesan, A. ORCID:, Gulea, Mihaela and Bonnet, Dominique (2020) Three cheers for nitrogen: aza-DKPs, the aza analogues of 2,5-diketopiperazines. RSC Advances, 10 (71). pp. 43358-43370. ISSN 2046-2069

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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.

Item Type: Article
Faculty \ School: Faculty of Science > School of Pharmacy
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Depositing User: LivePure Connector
Date Deposited: 09 Jan 2021 01:22
Last Modified: 22 Oct 2022 07:38
DOI: 10.1039/D0RA09457A

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