Synthesis and carbonic anhydrase I, II, VII, and IX inhibition studies with a series of benzo[d]thiazole-5- and 6-sulfonamides

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ID: 70177
2017
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Abstract
A series of benzo[d]thiazole-5- and 6-sulfonamides has been synthesized and investigated for the inhibition of several human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms, using ethoxzolamide (EZA) as lead molecule. 2-Amino-substituted, 2-acylamino- and halogenated (bromo-and iodo-derivatives at the heterocyclic ring) compounds led to several interesting inhibitors against the cytosolic hCA I, II and VII, as well as the transmembrane, tumor-associated hCA IX isoforms. Several subnanomolar/low nanomolar, isoform-selective sulfonamide inhibitors targeting hCA II, VII and IX were detected. The sharp structure–activity relationship for CA inhibition with this small series of derivatives, with important changes of activity observed even after minor changes in the scaffold or at the 2-amino moiety, make this class of scarcely investigated sulfonamides of particular interest for further investigations.
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abdoli2017synthesisjournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Abdoli, Morteza;Angeli, Andrea;Bozdag, Murat;Carta, Fabrizio;Kakanejadifard, Ali;Saeidian, Hamid;Supuran, Claudiu T.;
Journal Journal of enzyme inhibition and medicinal chemistry
Year 2017
DOI
DOI not found
URL
http://dx.doi.org/10.1080/14756366.2017.1356295
Keywords
Therapeutics. Pharmacology Medicine Science

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