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Carbonic anhydrase inhibitory properties of novel sulfonamide derivatives of aminoindanes and aminotetralins

机译:氨基茚满和氨基四氢萘的新型磺酰胺衍生物的碳酸酐酶抑制特性

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摘要

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 (K-i = 46 +/- 5.4 mu M, r(2) = 0.978), N-(1,2,3,4-tetrahydronaphthalene-2-yl) methanesulfonamide was found to have the best inhibitory effect against hCA II (K-i = 94 +/- 7.6 mu M, r(2) = 0.982).
机译:合成了源自茚满和四氢呋喃的六种磺酰胺。测定了合成磺酰胺的人碳酸酐酶同工酶hCA I和hCA II抑制作用。从这些化合物中,N-(5,6-二甲氧基-2,3-二氢-1H-茚满-2-基)甲烷磺酰胺显示出对hCA I的最强抑制作用(Ki = 46 +/- 5.4μM, r(2)= 0.978),N-(1,2,3,4-四氢萘-2-基)甲磺酰胺被发现对hCA II具有最佳的抑制作用(Ki = 94 +/- 7.6μM,r( 2)= 0.982)。

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