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新型氨基茚满和氨基四氢萘磺胺衍生物的碳酸酐酶抑制特性。

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

机构信息

Faculty of Science, Department of Chemistry, Atatürk University , Erzurum , Turkey .

出版信息

J Enzyme Inhib Med Chem. 2014 Feb;29(1):35-42. doi: 10.3109/14756366.2012.750311. Epub 2013 Jan 12.

DOI:10.3109/14756366.2012.750311
PMID:23311862
Abstract

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).

摘要

合成了 6 种源自茚烷和四氢萘的磺酰胺类化合物。测定了合成的磺酰胺类化合物对人碳酸酐酶同工酶 hCA I 和 hCA II 的抑制作用。在这些化合物中,N-(5,6-二甲氧基-2,3-二氢-1H-茚-2-基)甲磺酰胺对 hCA I 的抑制作用最强(Ki=46±5.4µM,r(2)=0.978),N-(1,2,3,4-四氢萘-2-基)甲磺酰胺对 hCA II 的抑制作用最好(Ki=94±7.6µM,r(2)=0.982)。

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