Phosphinic acid-based enzyme inhibitors. (22nd June 2022)

• Record Type: Journal Article
• Authors: Vassiliou, Stamatia; Pagoni, Aikaterini; Węglarz-Tomczak, Ewelina; Talma, Michał; Tabor, Wojciech; Grabowiecka, Agnieszka; Berlicki, Łukasz; Mucha, Artur
• Is Part Of: Phosphorus, sulfur, and silicon and the related elements. Volume 197:Number 5/6(2022)
• Page Start: 451
• Page End: 456
• Publication Date: 2022-06-22
• Subjects: Organophosphorus compounds -- enzyme inhibitors -- aminopeptidases -- urease -- synthesis -- biological activity -- molecular modeling; Sulfur compounds -- Periodicals; Organosulfur compounds -- Periodicals; Phosphorus compounds -- Periodicals; Organophosphorus compounds -- Periodicals; Silicon compounds -- Periodicals; Organosilicon compounds -- Periodicals; 546
• DOI: 10.1080/10426507.2021.2011882
• Languages: English
• ISSNs: 1042-6507

Abstract

Abstract: The phosphinic acid functionality has emerged as an invaluable scaffold for the construction of biologically active compounds, in particular enzyme inhibitors. This article presents two examples of recent achievements in the preparation and application of phosphinic acids as ligands for hydrolases. Synthetic approaches to a dipeptide analog inhibitor of metalloaminopeptidases and a catechol-based inhibitor of urease are shown. The activity and mode of binding of phosphinic compounds to enzymes are further discussed. Graphical Abstract: UF0001