Synthesis and structure-activity relationships of novel benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II.
Synthesis and structure-activity relationships of novel benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II.
复制标题
对牛碳酸酐酶 II 具有强亲和力的新型苯磺酰胺的合成及其构效关系。
DOI：
10.1016/j.bmcl.2005.08.113
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发表时间：
2005
影响因子：
2.7
通讯作者：
P. Healy
中科院分区：
文献类型：
--
作者：
S. Poulsen;L. Bornaghi;P. Healy
该手稿报告了一系列新型单苯磺酰胺和双苯磺酰胺的鉴定，这些单苯磺酰胺对牛碳酸酐酶 II (bCAII) 具有强大的结合亲和力。这些化合物表现出纳摩尔平衡解离常数，Ki 范围为 4.7 至 9.3nM。所有化合物都是弱亲和力 bCAII 抑制剂 4-羧基苯磺酰胺的酯衍生物。讨论了这一系列新型化合物的结构-活性关系。
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 Ki’s ranging from 4.7 to 9.3nM. All compounds were ester derivatives of the weak affinity bCAII inhibitor, 4-carboxybenzenesulfonamide. Structure–activity relationships for this novel series of compounds are discussed.