title: Synthesis and carbonic anhydrase inhibitory properties of novel chalcone substituted benzenesulfonamides.
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.
authors.affiliation: Technical Sciences Vocational School, Giresun University, 28049 Giresun, Turkey. Electronic address: tayfunars28@hotmail.com.
authors.forename: Tayfun
authors.initials: T
authors.lastname: Arslan
authors.affiliation: Ağrı İbrahim Çeçen University, Department of Pharmaceutical Technology, 04100 Ağrı, Turkey.
authors.forename: Emir Alper
authors.initials: EA
authors.lastname: Türkoğlu
authors.affiliation: Ağrı İbrahim Çeçen University, Science and Art Faculty, Chemistry Department, 04100 Ağrı, Turkey. Electronic address: senturkm36@gmail.com.
authors.forename: Murat
authors.initials: M
authors.lastname: Şentürk
authors.affiliation: Universitá degli Studi di Firenze, Dipartimento Neurofarba, Sezione di Scienze, Polo Scientifico, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. Electronic address: claudiu.supuran@unifi.it.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D024401:Carbonic Anhydrase I / Q000378:metabolism*; D024402:Carbonic Anhydrase II / Q000378:metabolism*; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002599:Chalcone / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000096926:Benzenesulfonamides
chemical_list: D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II; D002257:Carbonic Anhydrase Inhibitors; D002599:Chalcone; D013449:Sulfonamides; D000096926:Benzenesulfonamides
keywords: Carbonic anhydrase; Chalcone; Inhibitors; Sulfonamides