三种新型芳香磺胺类碳酸酐酶 I、II、IV 和 XII 的抑制剂。
Three new aromatic sulfonamide inhibitors of carbonic anhydrases I, II, IV and XII.
机构信息
Dipartimento di Chimica, Università di Firenze, Via della Lastruccia, Sesto Fiorentino (Firenze), Italy.
出版信息
J Enzyme Inhib Med Chem. 2013 Apr;28(2):289-93. doi: 10.3109/14756366.2011.649269. Epub 2012 Feb 3.
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 (IC(50)) 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.
4-磺胺酰基-N-(3-吗啉丙基)苯甲酰胺（I-1）、N-(3-吗啉丙基)苯-1,4-二磺酰胺（I-2）和 N-(4-二乙氨基乙氧基苄基)苯-1,4-双磺酰胺（I-3）被制备并作为四种碳酸酐酶（CA）同工酶 hCA I、hCA II、hCA IV 和 hCA XII 的抑制剂进行了检测。这些化合物的半数最大抑制浓度（IC(50)）范围为 58 至 740nmol/L。三种芳基磺酰胺对所研究的同工酶表现出不同的活性，对同工酶 hCA XII 的亲和力最低。
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