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

Autor: Maujean T; Université de Strasbourg, CNRS, Laboratoire d'Innovation Thérapeutique, LabEX MEDALIS, Faculté de Pharmacie LIT UMR 7200 Strasbourg F-67000 France dominique.bonnet@unistra.fr gulea@unistra.fr., Girard N; Université de Strasbourg, CNRS, Laboratoire d'Innovation Thérapeutique, LabEX MEDALIS, Faculté de Pharmacie LIT UMR 7200 Strasbourg F-67000 France dominique.bonnet@unistra.fr gulea@unistra.fr., Ganesan A; School of Pharmacy, University of East Anglia Norwich Research Park Norwich NR4 7TJ UK., Gulea M; Université de Strasbourg, CNRS, Laboratoire d'Innovation Thérapeutique, LabEX MEDALIS, Faculté de Pharmacie LIT UMR 7200 Strasbourg F-67000 France dominique.bonnet@unistra.fr gulea@unistra.fr., Bonnet D; Université de Strasbourg, CNRS, Laboratoire d'Innovation Thérapeutique, LabEX MEDALIS, Faculté de Pharmacie LIT UMR 7200 Strasbourg F-67000 France dominique.bonnet@unistra.fr gulea@unistra.fr.
Jazyk: angličtina
Zdroj: RSC advances [RSC Adv] 2020 Dec 07; Vol. 10 (71), pp. 43358-43370. Date of Electronic Publication: 2020 Dec 07 (Print Publication: 2020).
DOI: 10.1039/d0ra09457a
Abstrakt: 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.
Competing Interests: There are no conflicts to declare.
(This journal is © The Royal Society of Chemistry.)
Databáze: MEDLINE