title: Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes.
abstract: In the current study, a series of pyrazole-sulfonamide derivatives (2-14) were synthesized, characterized, and the inhibition effects of the derivatives on human carbonic anhydrases (hCA I and hCA II) were investigated as in vitro. Structures of these sulfonamides were confirmed by FT-IR, (1)H NMR, (13)C NMR and LC-MS analysis. (1)H NMR and (13)C NMR revealed the tautomeric structures. hCA I and hCA II isozymes were purified from human erythrocytes and inhibitory effects of newly synthesized sulfonamides on esterase activities of these isoenzymes have been studied. The K(i) values of compounds were 0.062-1.278 μM for hCA I and 0.012-0.379 μM for hCA II. The inhibition effects of 7 for hCA I and 4 for hCA II isozymes were almost in nanomolar concentration range.
authors.affiliation: Dumlupinar University, Art and Science Faculty, Department of Chemistry, 43100 Kütahya, Turkey.
authors.forename: Havva
authors.initials: H
authors.lastname: Balseven
authors.forename: M
authors.initials: M
authors.lastname: Mustafa İşgör
authors.forename: Samet
authors.initials: S
authors.lastname: Mert
authors.forename: Zuhal
authors.initials: Z
authors.lastname: Alım
authors.forename: Sükrü
authors.initials: S
authors.lastname: Beydemir
authors.forename: Salim
authors.initials: S
authors.lastname: Ok
authors.forename: Rahmi
authors.initials: R
authors.lastname: Kasımoğulları
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*; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D008958:Models, Molecular; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D011720:Pyrazoles; D013449:Sulfonamides; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II