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

被引:124
作者
Akbaba, Yusuf [1 ]
Akincioglu, Akin [1 ]
Gocer, Hulya [1 ,2 ]
Goksu, Suleyman [1 ]
Gulcin, Ilhami [1 ]
Supuran, Claudiu T. [3 ]
机构
[1] Ataturk Univ, Fac Sci, Dept Chem, TR-25240 Erzurum, Turkey
[2] Ibrahim Cecen Univ Agri, Cent Researching Lab, Agri, Turkey
[3] Univ Florence, Chim Bioorgan Lab, Florence, Italy
关键词
Aminoindane; aminotetralin; carbonic anhydrase; enzyme inhibition; sulfonamide; ERYTHROCYTE ISOZYMES I; VITRO; ACETAZOLAMIDE; PURIFICATION; DANTROLENE; MELATONIN; SERIES; ACID; QSAR;
D O I
10.3109/14756366.2012.750311
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
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).
引用
收藏
页码:35 / 42
页数:8
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