Structures and Biological Activities of Diketopiperazines from Marine Organisms: A Review

Diketopiperazines are potential structures with extensive biological functions, which have attracted much attention of natural product researchers for a long time. These compounds possess a stable six-membered ring, which is an important pharmacophore. The marine organisms have especially been proven to be a wide source for discovering diketopiperazine derivatives. In recent years, more and more interesting bioactive diketopiperazines had been found from various marine habitats. This review article is focused on the new 2,5-diketopiperazines derived from marine organisms (sponges and microorganisms) reported from the secondary half-year of 2014 to the first half of the year of 2021. We will comment their chemical structures, biological activities and sources. The objective is to assess the merit of these compounds for further study in the field of drug discovery.

Automated summary

Diketopiperazines are compounds with extensive biological functions and a stable six-membered ring, making them important for drug discovery. Marine organisms have been a key source for discovering diketopiperazine derivatives, with an increasing number of bioactive diketopiperazines being found in recent years. This review focuses on new 2,5-diketopiperazines derived from marine organisms, evaluating their chemical structures, biological activities, and sources for potential further study in drug discovery.