Ebselen and Analogues: Pharmacological Properties and Synthetic Strategies for Their Preparation

Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.

Automated summary

Ebselen, the leader of selenorganic compounds, has been identified as a mimetic of the key antioxidant enzyme glutathione peroxidase and is currently undergoing clinical evaluation for treating COVID-19 patients. Despite its lack of specificity in vitro, Ebselen has shown good tolerance in vivo with no signs of toxicity at administered doses. Additionally, there is a lack of review articles on synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold, a topic which is addressed in this review.