4.5 Article

Selenocarbamates As a Prodrug-Based Approach to Carbonic Anhydrase Inhibition

期刊

CHEMMEDCHEM
卷 17, 期 11, 页码 -

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202200085

关键词

selenocarbamates; carbonic anhydrase inhibitors; X-ray crystallography; inhibition mechanism; selenium

资金

  1. Italian Ministry for University and Research (MIUR) [2017XYBP2R]
  2. Universita degli Studi di Firenze within the CRUI-CARE Agreement

向作者/读者索取更多资源

This study presents the activity of selenocarbamates as novel carbonic anhydrase (CA) inhibitors. Through CA-mediated hydrolysis, selenocarbamates release selenolates that effectively inhibit CA by binding to zinc. Different human CA isoforms were evaluated against a series of selenocarbamates with high molecular diversity and complexity. X-ray studies provided insights into the binding mode of this novel class of CA inhibitors.
A study on the activity of selenocarbamates as a novel chemotype acting as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors is reported. Undergoing CA-mediated hydrolysis, selenocarbamates release selenolates behaving as zinc binding groups and effectively inhibiting CAs. A series of selenocarbamates characterised by high molecular diversity and complexity have been studied against different human CA isoforms such as hCA I, II, IX and XII. Selenocarbamates behave as masked selenols with potential biological applications as prodrugs for CAs inhibition-based strategies. X-ray studies provided insights into the binding mode of this novel class of CA inhibitors.

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