title: Synthesis and evaluation of sulfonamide-bearing thiazole as carbonic anhydrase isoforms hCA I and hCA II.
abstract: Sulfonamide-bearing thiazole compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of the 12 synthesized sulfonamide (5a-l) on the hydratase and esterase activities of these isoenzymes (hCA-I and hCA-II) were studied in vitro. In relation to these activities, the inhibition equilibrium constants (Ki) were determined. The results showed that all the synthesized compounds inhibited the CA isoenzyme activity. Among them 5b was found to be the most active (IC50 = 0.35 μM; Ki: 0.33 μM) for hCA I and hCA II.
authors.affiliation: a Chemistry Department, Faculty of Arts and Sciences, Sakarya University , Sakarya , Turkey and.
authors.forename: Soner
authors.initials: S
authors.lastname: Kılıcaslan
authors.affiliation: a Chemistry Department, Faculty of Arts and Sciences, Sakarya University , Sakarya , Turkey and.
authors.forename: Mustafa
authors.initials: M
authors.lastname: Arslan
authors.affiliation: a Chemistry Department, Faculty of Arts and Sciences, Sakarya University , Sakarya , Turkey and.
authors.forename: Zeynep
authors.initials: Z
authors.lastname: Ruya
authors.affiliation: b Chemistry Department, Faculty of Arts and Sciences, Balikesir University , Balikesir , Turkey.
authors.forename: Çigdem
authors.initials: Ç
authors.lastname: Bilen
authors.affiliation: b Chemistry Department, Faculty of Arts and Sciences, Balikesir University , Balikesir , Turkey.
authors.forename: Adem
authors.initials: A
authors.lastname: Ergün
authors.affiliation: b Chemistry Department, Faculty of Arts and Sciences, Balikesir University , Balikesir , Turkey.
authors.forename: Nahit
authors.initials: N
authors.lastname: Gençer
authors.affiliation: b Chemistry Department, Faculty of Arts and Sciences, Balikesir University , Balikesir , Turkey.
authors.forename: Oktay
authors.initials: O
authors.lastname: Arslan
mesh_terms: D066241:Carbon-13 Magnetic Resonance Spectroscopy; D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors*; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors*; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D062105:Molecular Docking Simulation; D066244:Proton Magnetic Resonance Spectroscopy; D013055:Spectrophotometry, Infrared; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*; D013844:Thiazoles / Q000737:chemistry*
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D013449:Sulfonamides; D013844:Thiazoles; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II
keywords: Carbonic anhydrase; enzyme inhibitor; sulfonamide; thiazole