Carbonic anhydrase inhibitory properties of novel sulfonamide derivatives of aminoindanes and aminotetralins
Yusuf Akbaba, Akın Akıncıoğlu, Hülya Göçer, Süleyman Göksu, İlhami Gülçın, Claudiu T. Supuran
Abstract
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Yusuf Akbaba, Akın Akıncıoğlu, Hülya Göçer, Süleyman Göksu, İlhami Gülçın, Claudiu T. Supuran
Abstract
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Six sulfonamides derived from indanes and tetralines were synthesized. The human carbonic anhydrase isozymes hCA I and hCA II inhibition effects of the synthesized sulfonamides were determined. From these compounds, while N-(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methane sulfonamide showed the most potent inhibitory effect against hCA I (Ki=46 ± 5.4 µM, r(2) =0.978), N-(1,2,3,4-tetrahydronaphthalene-2-yl)methanesulfonamide was found to have the best inhibitory effect against hCA II (Ki=94 ± 7.6 µM, r(2) =0.982).
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Six sulfonamides derived from indanes and tetralines were synthesized. The human carbonic anhydrase isozymes hCA I and hCA II inhibition effects of the synthesized sulfonamides were determined. From these compounds, while N-(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl)methane sulfonamide showed the most potent inhibitory effect against hCA I (Ki=46 ± 5.4 µM, r(2) =0.978), N-(1,2,3,4-tetrahydronaphthalene-2-yl)methanesulfonamide was found to have the best inhibitory effect against hCA II (Ki=94 ± 7.6 µM, r(2) =0.982).
Key concepts: Sulfonamide, Carbonic anhydrase, Chemistry, Carbonic Anhydrase I, Isozyme, Inhibitory postsynaptic potential, Enzyme inhibition, Enzyme