Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes
Autor(en): | Balseven, Havva Isgor, M. Mustafa Mert, Samet Alim, Zuhal Beydemir, Sukru Ok, Salim Kasimogullari, Rahmi |
Stichwörter: | 5-AMINO-1,3,4-THIADIAZOLE-2-SULFONAMIDE DERIVATIVES; Biochemistry & Molecular Biology; Carbonic anhydrase; Chemistry; Chemistry, Medicinal; Chemistry, Organic; DESIGN; Diazonium; ERYTHROCYTES IN-VITRO; Inhibition; Pharmacology & Pharmacy; Pyrazole; Sulfonamide | Erscheinungsdatum: | 2013 | Herausgeber: | PERGAMON-ELSEVIER SCIENCE LTD | Enthalten in: | BIOORGANIC & MEDICINAL CHEMISTRY | Band: | 21 | Ausgabe: | 1 | Startseite: | 21 | Seitenende: | 27 | Zusammenfassung: | 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, H-1 NMR, C-13 NMR and LC-MS analysis. H-1 NMR and C-13 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 mu M for hCA I and 0.012-0.379 mu M for hCA II. The inhibition effects of 7 for hCA I and 4 for hCA II isozymes were almost in nanomolar concentration range. Published by Elsevier Ltd. |
ISSN: | 09680896 | DOI: | 10.1016/j.bmc.2012.11.012 |
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geprüft am 09.06.2024