Synthesis and structure–activity relationships of novel benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II

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• 作者：Sally-Ann Poulsen ; Laurent F. Bornaghi and Peter C. Healy
• 关键词：Carbonic anhydrase ; Sulfonamides
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：2005
• 卷：15
• 期：24
• 页码：5429-5433
• 文件大小：133 K

摘要

This manuscript reports the identification of a novel series of mono- and bis- benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II (bCAII). These compounds exhibited nanomolar equilibrium dissociation constants with K_i’s ranging from 4.7 to 9.3 nM. All compounds were ester derivatives of the weak affinity bCAII inhibitor, 4-carboxybenzenesulfonamide. Structure–activity relationships for this novel series of compounds are discussed.