Diketopiperazines (DKPs) are mainly produced by microorganisms. In recent years, active natural products with DKPs structure have been isolated from marine bacteria, actinomycetes and fungi. The stable six-membered ring framework makes DKPs a vital pharmacophore in medicinal chemistry. Several recent studies have demonstrated that it has antibacterial, antifungal, antiviral, antitumor, immunosuppressive, neuroprotective, anti-malaria, anti-prion, and anti-hyperglycemia properties. Some DKPs are signaling molecules for intercellular communication, which can activate or inhibit bacterial Lux R-mediated quorum sensing. They are considered potential new anti-infective drugs that could control biofilm formation by interfering with information communication between microbes. DKPs possess excellent biological activities and have received extensive attention from medicinal chemistry workers. Bioactivity studies of DKPs have revealed that many highly active lead compounds exist in antibacterial, antitumor, and antiviral fields and in treating neurological disorders. This paper reviews the research progress of diketopiperazines in the past ten years.

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二酮哌嗪类化合物的活性及生物合成研究进展

二酮哌嗪（DKP）主要由微生物产生。近年来，人们从海洋细菌、放线菌和真菌中分离出了具有DKPs结构的活性天然产物。稳定的六元环框架使 DKP 成为药物化学中重要的药效团。最近的几项研究表明，它具有抗菌、抗真菌、抗病毒、抗肿瘤、免疫抑制、神经保护、抗疟疾、抗朊病毒和抗高血糖特性。一些 DKP 是细胞间通讯的信号分子，可以激活或抑制细菌 Lux R 介导的群体感应。它们被认为是潜在的新型抗感染药物，可以通过干扰微生物之间的信息通讯来控制生物膜的形成。DKPs具有优异的生物活性，受到药物化学工作者的广泛关注。DKP 的生物活性研究表明，许多高活性先导化合物存在于抗菌、抗肿瘤、抗病毒领域以及治疗神经系统疾病中。本文综述了近十年来二酮哌嗪类药物的研究进展。