A class of sulfonamides as carbonic anhydrase I and II inhibitors

被引:47
|
作者
Gokcen, Taner [1 ,2 ]
Gulcin, Ilhami [3 ,4 ]
Ozturk, Turan [1 ,2 ]
Goren, Ahmet C. [1 ]
机构
[1] TUBITAK UME, Chem Grp Labs, POB 54, TR-41470 Gebze, Kocaeli, Turkey
[2] Istanbul Tech Univ, Dept Organ Chem, Fac Sci, Istanbul, Turkey
[3] Ataturk Univ, Dept Chem, Fac Sci, Erzurum, Turkey
[4] King Saud Univ, Dept Zool, Coll Sci, Fetal Programming Dis Res Chair, Riyadh, Saudi Arabia
关键词
Enzyme inhibition; gallic acid; p-hydroxybenzoic acid; MESSENGER-RNA EXPRESSION; ISOENZYMES I; ENZYME-ACTIVITY; CDNA CLONING; DRUG DESIGN; HCA I; DERIVATIVES; VITRO; VIVO; ANTIOXIDANT;
D O I
10.1080/14756366.2016.1198900
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Four groups of novel sulfonamide derivatives: (i) acetoxybenzamide, (ii) triacetoxybenzamide, (iii) hydroxybenzamide and (iv) trihydroxybenzamide, all having thiazole, pyrimidine, pyridine, isoxazole and thiadiazole moieties were prepared and their inhibitory effects were studied on two metalloenzymes, i.e. carbonic anhydrase isozymes (hCA I and II), purified from human erythrocyte cells by Sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography. These enzymes are present in almost all living organisms to catalyse the synthesis of bicarbonate ion (HCO3-) from carbon dioxide and water. The sulfonamide derivatives were found to be active against hCA I and II in the range of 2.62-136.54 and 5.74-210.58nM, respectively.
引用
收藏
页码:180 / 188
页数:9
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