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Synthesis and carbonic anhydrase inhibitory properties of new spiroindoline-substituted sulphonamide compounds.
Archives of Physiology and Biochemistry 2017 December
New spiroindoline-substituted sulphonamide compounds were synthesised and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of the 14 synthesised sulphonamides (6a-n) on esterase activities of these isoenzymes were studied in vitro. In relation to these activities, the inhibition equilibrium constants (Ki ) were determined. The results showed that all the synthesised compounds inhibited the carbonic anhydrase (CA) isoenzyme activity. Among them, 6b was found to be the most active (Ki : 0.042 μM) for hCA I and 6a (Ki : 0.151 μM) for hCA II.
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