Microwave-assisted synthesis and bioevaluation of new sulfonamides |
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Authors: | Halise Inci Gul Cem Yamali Fatma Yesilyurt Hiroshi Sakagami Kaan Kucukoglu Ilhami Gulcin |
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Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ataturk University, Erzurum, Turkey;2. Division of Pharmacology, Meikai University School of Dentistry, Sakado, Saitama, Japan;3. Department of Chemistry, Faculty of Science, Ataturk University, Erzurum, Turkey;4. Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia |
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Abstract: | In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13C NMR and HRMS. Cytotoxic activities and inhibitory effects on carbonic anhydrase I and II isoenzymes of the compounds were investigated. The compounds 9 (PSE?=?4.2), 12 (PSE?=?4.1) and 13 (PSE?=?3.9) with the highest potency selectivity expression (PSE) values in cytotoxicity experiments and the compounds 13 (Ki?=?3.73?±?0.91?nM toward hCA I) and 14 (Ki?=?3.85?±?0.57?nM toward hCA II) with the lowest Ki values in CA inhibition studies can be considered as leader compounds for further studies. |
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Keywords: | Carbonic anhydrase cytotoxicity microwave pyrazoline sulfonamide |
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