Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes involved in many bioprocesses, through catalysis of the reversible hydration/dehydration process of CO2/HCO3-. The inhibition of human CA isoforms I and II with a new series of sulfonamide derivatives incorporating substituted chalcone moieties were studied in this study. All these newly synthesized sulfonamides demonstrated important inhibitory profiles to these CA isoforms with KIs in the range of 9.88 to 55.43nM, making these compounds interesting leads, with potential applications in medicinal chemistry.

Synthesis and carbonic anhydrase inhibitory properties of novel chalcone substituted benzenesulfonamides / Arslan, Tayfun; Türkoğlu, Emir Alper; Şentürk, Murat; Supuran, Claudiu T.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 26:(2016), pp. 5867-5870. [10.1016/j.bmcl.2016.11.017]

Synthesis and carbonic anhydrase inhibitory properties of novel chalcone substituted benzenesulfonamides

SUPURAN, CLAUDIU TRANDAFIR
2016

Abstract

Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes involved in many bioprocesses, through catalysis of the reversible hydration/dehydration process of CO2/HCO3-. The inhibition of human CA isoforms I and II with a new series of sulfonamide derivatives incorporating substituted chalcone moieties were studied in this study. All these newly synthesized sulfonamides demonstrated important inhibitory profiles to these CA isoforms with KIs in the range of 9.88 to 55.43nM, making these compounds interesting leads, with potential applications in medicinal chemistry.
2016
26
5867
5870
Arslan, Tayfun; Türkoğlu, Emir Alper; Şentürk, Murat; Supuran, Claudiu T.
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1075101
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