期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 32, 期 1, 页码 189-192出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2016.1244533
关键词
Carbonic anhydrase; enzyme; pyrazoline; sulfonamide
资金
- Ataturk University
- Ataturk University Research Found, Turkey [2013/289]
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.
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