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Calixarenes Incorporating Sulfonamide Moieties: Versatile Ligands for Carbonic Anhydrases Inhibition. | LitMetric

Calixarenes Incorporating Sulfonamide Moieties: Versatile Ligands for Carbonic Anhydrases Inhibition.

Chemistry

Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Via U. Schiff 6, 50019, Sesto Fiorentino, Firenze, Italy.

Published: January 2022

AI Article Synopsis

  • Carbonic anhydrases (CAs) are important targets for drug development due to their role in various diseases, highlighting the need for selective inhibitors that can differentiate between CA isoforms.* -
  • Researchers successfully synthesized new ligands by combining calixarenes with benzensulfonamide, resulting in inhibitors that showed effective targeting of human CA isoforms with nanomolar activity and promising selectivity.* -
  • X-ray and molecular modeling studies revealed how these calixarene derivatives bind to their targets, paving the way for future design of multifunctional inhibitors that can tackle multiple pathological issues.*

Article Abstract

Carbonic anhydrases (CAs) continue to represent a relevant pharmaceutical target. The need of selective inhibitors and the involvement of these metalloenzymes in many multifaceted diseases boost the search for new ligands able to distinguish among the different CA isoforms, and for multifunctional systems simultaneously able to inhibit CAs and to interfere with other pathological events by interacting with additional targets. In this work, we successfully explored the possibility of preparing new CAs ligands by combining calixarenes with benzensulfonamide units. Inhibition tests towards three human CA isoforms evidenced, for some of the ligands, K values in the nanomolar range and promising selectivity. X-ray and molecular modeling studies provided information on the mode of binding of these calixarene derivatives. Thanks to the encouraging results and the structural features typical of the calixarene scaffold, it is then possible to plan for the future the design of multifunctional inhibitors for this class of widely spread enzymes.

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Source
http://dx.doi.org/10.1002/chem.202103527DOI Listing

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