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J Enzyme Inhib Med Chem. 2014 Feb;29(1):132-6. doi: 10.3109/14756366.2012.757603. Epub 2013 Jan 28.

Synthesis and carbonic anhydrase inhibitory properties of 1,3-dicarbonyl derivatives of methylaminobenzene-sulfonamide.

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Chemistry Department, Faculty of Arts and Sciences, Sakarya University , Sakarya, Turkey , and.


1,3-Dicarbonyl derivatives of methylaminobenzene-sulfonamide were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and hCA II were evaluated. hCA I and hCA II from human erythrocytes were purified by a simple one-step procedure by using Sepharose 4B-L-tyrosine-sulfanilamide affinity column. Our results show that the synthesized compounds inhibited the activity of carbonic anhydrase (CA) I and CA II. Among them, 2b and 2e were found to be the most active (IC50=2.12 and 2.52 µM) for hCA I and hCA II, respectively.

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