Three new aromatic sulfonamide inhibitors of carbonic anhydrases I, II, IV and XII

被引：58
作者：
Supuran, C. T. [1 ]
Maresca, A. [1 ]
Gregan, F. [2 ]
Remko, M. [3 ]
机构：
[1] Univ Florence, Dipartimento Chim, I-50144 Florence, Italy
[2] Matej Bell Univ, Fac Nat Sci, Dept Chem, Banska Bystrica, Slovakia
[3] Comenius Univ, Fac Pharm, Dept Pharmaceut Chem, Bratislava, Slovakia
来源：
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2013年 / 28卷 / 02期
关键词：
Aromatic sulfonamides; carbonic anhydrase inhibitors; glaucoma; GAS-PHASE ACIDITY; MOLECULAR-STRUCTURE; LIPOPHILICITY; SELECTIVITY; SOLUBILITY; BINDING; PK(A);
D O I：
10.3109/14756366.2011.649269
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：
4-Sulfamoyl-N-(3-morpholinopropyl)benzamide (I-1), N-(3-morpholinopropyl)benzene-1,4-disulfonamide (I-2) and N-(4-diethylaminoethoxybenzyl)benzene-1,4-bis(sulfonamide (I-3), were prepared and assayed as inhibitors of four carbonic anhydrase (CA) isoenzymes hCA I, hCA II, hCA IV and hCA XII. These compounds exhibited nanomolar half maximal inhibitory concentration (IC50) ranging from 58 to 740 nmol/L. All three aromatic sulfonamides show different activities for the isoenzymes studied with lowest affinity against isoenzyme hCA XII.
引用
收藏
页码：289 / 293
页数：5
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