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

Timothé Maujean, Nicolas Girard, A. Ganesan, Mihaela Gulea, Dominique Bonnet

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)
27 Downloads (Pure)


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.
Original languageEnglish
Pages (from-to)43358-43370
Number of pages13
JournalRSC Advances
Issue number71
Early online date7 Dec 2020
Publication statusPublished - 2020

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