Gliovirin家族:发现、抗菌活性和合成进展

Gliovirins: Discovery,Antimicrobial Activity and Synthesis

天然产物gliovirin家族是属于真菌次级代谢产物epipolythiodiketopiperazines (ETPs)中的一类特殊生物碱,除了特征性的α-,β-硫代二酮哌嗪桥环外,还包含一个高度官能团化的cis-1,2-恶嗪十氢萘并环.至今为止,该家族已有30余个结构被分离报道,大多具有重要的抗菌活性.其新颖的化学结构和多样的生理活性,吸引了合成化学家的广泛关注.介绍了该家族天然产物的分离鉴定、生理活性、初步的生理活性作用机制研究和生源关系,并对已知的全合成和1,2-恶嗪十氢萘骨架的构建策略进行了归纳总结.

The gliovirin family belongs to the structural subgroup of epipolythiodiketopiperazines(ETPs),a class of fungal alkaloids.The structure features a characteristic α-,β-thiodiketopiperazine bridge ring and a unique highly functionalized cis-1,2-oxazadecaline core.Up to now,more than 30 members have been characterized and most of them have shown significant antimicrobial activities.The important biological profile and complex architecture render them as the intriguing targets for the total synthesis.In this review,we summarized the isolation and structure determination,bioactivity,mode of action and biogenesis proposal,as well as the current status of total synthesis and novel method development to access the 1,2-oxazadecaline core.