Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes |
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| Authors: | Havva Balseven M Mustafa ??gör Samet Mert Zuhal Al?m ?ükrü Beydemir Salim Ok Rahmi Kas?mo?ullar? |
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| Institution: | 1. Dumlupinar University, Art and Science Faculty, Department of Chemistry, 43100 Kütahya, Turkey;2. Ataturk University, Faculty of Sciences, Department of Chemistry, Biochemistry Division, 25240 Erzurum, Turkey;3. Institut für Chemie, Barbarastr. 7, Universität Osnabrück, 49069 Osnabrück, Germany;4. King Fahd University of Petroleum and Minerals (KFUPM), Faculty of Natural Sciences, Chemistry Department, 31261-5048 Dhahran, Saudi Arabia |
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| 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, 1H NMR, 13C NMR and LC–MS analysis. 1H NMR and 13C 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 Ki 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. |
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