4-取代-2-噻吩磺酰胺的合成及其碳酸酐酶抑制活性
Synthesis and carbonic anhydrase inhibitory activity of 4-substituted 2-thiophenesulfonamides.
作者信息
Holmes J M, Lee G C, Wijono M, Weinkam R, Wheeler L A, Garst M E
机构信息
Department of Chemical Sciences, Allergan Inc., Irvine, California 92715.
出版信息
J Med Chem. 1994 May 27;37(11):1646-51. doi: 10.1021/jm00037a015.
PMID:8201598
Abstract
A series of 4-substituted 2-thiophenesulfonamides was prepared from 3-thiophenecarboxaldehyde using metalation chemistry developed for 3-furaldehyde. Several of these compounds inhibit carbonic anhydrase II in vitro at concentrations of less than 10 nM. In addition, none of these compounds exhibit sensitization potential as determined from in vitro measurement of cysteine reactivity.
摘要
利用为3-呋喃甲醛开发的金属化化学方法，从3-噻吩甲醛制备了一系列4-取代的2-噻吩磺酰胺。其中几种化合物在体外浓度低于10 nM时可抑制碳酸酐酶II。此外，根据半胱氨酸反应性的体外测量结果，这些化合物均无致敏潜力。
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