Synthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines
| Autor: | Ebru Mete, Claudiu T. Supuran, Parham Taslimi, Halise Inci Gul, İlhami Gülçin |
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| Přispěvatelé: | Bartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümü |
| Jazyk: | angličtina |
| Rok vydání: | 2017 |
| Předmět: |
Carbonic Anhydrase I
Stereochemistry Proton Magnetic Resonance Spectroscopy Pyrazoline Carbonic Anhydrase II 01 natural sciences Mass Spectrometry chemistry.chemical_compound Carbonic anhydrase Drug Discovery sulfonamide medicine Carbon-13 Magnetic Resonance Spectroscopy Carbonic Anhydrase Inhibitors pyrazoline Pharmacology chemistry.chemical_classification biology 010405 organic chemistry lcsh:RM1-950 General Medicine Carbon-13 NMR 0104 chemical sciences Sulfonamide 010404 medicinal & biomolecular chemistry enzyme Enzyme lcsh:Therapeutics. Pharmacology chemistry Proton NMR biology.protein Pyrazoles Original Article Acetazolamide medicine.drug |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 189-192 (2017) Journal of Enzyme Inhibition and Medicinal Chemistry |
| ISSN: | 1475-6374 1475-6366 |
| Popis: | 4-(3-(4-Substituted-phenyl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl) benzenesulfonamides (9-16) were successfully synthesized and their chemical structures were confirmed by H-1 NMR, C-13 NMR, and HRMS spectra. Carbonic anhydrase I and II inhibitory effects of the compounds were investigated. Ki values of the compounds were in the range of 316.7 +/- 9.6-533.1 +/- 187.8nM towards hCA I and 412.5 +/- 115.4-624.6 +/- 168.2nM towards hCA II isoenzymes. While K-i values of the reference compound Acetazolamide were 278.8 +/- 44.3 nM and 293.4 +/- 46.4 nM towards hCA I and hCA II izoenzymes, respectively. Compound 14 with bromine and compound 13 with fluorine substituents can be considered as the leader compounds of the series because of the lowest K-i values in series to make further detailed carbonic anhydrase inhibiton studies. |
| Databáze: | OpenAIRE |
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