Phosphinic acid-based enzyme inhibitors

被引:1
|
作者
Vassiliou, Stamatia [1 ]
Pagoni, Aikaterini [1 ]
Weglarz-Tomczak, Ewelina [2 ]
Talma, Michal [2 ]
Tabor, Wojciech [2 ]
Grabowiecka, Agnieszka [2 ]
Berlicki, Lukasz [2 ]
Mucha, Artur [2 ]
机构
[1] Univ Athens, Dept Chem, Lab Organ Chem, Athens, Greece
[2] Wroclaw Univ Sci & Technol, Dept Bioorgan Chem, Fac Chem, Wroclaw, Poland
关键词
Organophosphorus compounds; enzyme inhibitors; aminopeptidases; urease; synthesis; biological activity; molecular modeling; LEUCINE AMINOPEPTIDASE; STRUCTURAL BASIS; UREASE; DIPEPTIDE; POTENT; DERIVATIVES; PEPTIDES; TARGETS;
D O I
10.1080/10426507.2021.2011882
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
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.
引用
收藏
页码:451 / 456
页数:6
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