Litcius/Paper detail

Selenocarbamates As a Prodrug‐Based Approach to Carbonic Anhydrase Inhibition

Andrea Angeli, Marta Ferraroni, Antonella Capperucci, Damiano Tanini, Gabriele Costantino, Claudiu T. Supuran

2022ChemMedChem22 citationsDOIOpen Access PDF

Abstract

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.

Topics & Concepts

Carbonic anhydraseProdrugCarbonic anhydrase IIChemistryEnzymeBiochemistryChemotypeZincHydrolysisCombinatorial chemistryStereochemistryPharmacologyBiologyOrganic chemistryEssential oilChromatographyEnzyme function and inhibitionCholinesterase and Neurodegenerative DiseasesSynthesis and Catalytic Reactions