Maujean Timothé, Girard Nicolas, Ganesan A, Gulea Mihaela, Bonnet Dominique
Université de Strasbourg, CNRS, Laboratoire d'Innovation Thérapeutique, LabEX MEDALIS, Faculté de Pharmacie LIT UMR 7200 Strasbourg F-67000 France
School of Pharmacy, University of East Anglia Norwich Research Park Norwich NR4 7TJ UK.
RSC Adv. 2020 Dec 7;10(71):43358-43370. doi: 10.1039/d0ra09457a. eCollection 2020 Nov 27.
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.
含氮杂环是药理学探针和候选药物的主要来源。为了扩展其分子多样性及其潜在的生物活性，设计和合成新的氮杂环骨架具有重要意义。因此，氮杂二酮哌嗪（aza-DKPs）作为著名的2,5-二酮哌嗪（DKPs）的氮杂类似物，成为一种有前景的新骨架。尽管氮杂二酮哌嗪的首次合成可追溯到1951年，但在过去十年中取得了重大进展。这篇专题文章总结了合成氮杂二酮哌嗪并使其功能化的不同策略。还讨论了它们的生物学特性以及在药物化学和药物发现中的潜在应用。
