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碳酸酐酶抑制剂:芳香族和杂环磺酰胺的席夫碱及其金属配合物。

Carbonic anhydrase inhibitors: Schiff's bases of aromatic and heterocyclic sulfonamides and their metal complexes.

作者信息

Chohan Zahid H, Scozzafava Andrea, Supuran Claudiu T

机构信息

Department of Chemistry, Islamia University, Bahawalpur, Pakistan.

出版信息

J Enzyme Inhib Med Chem. 2004 Jun;19(3):263-7. doi: 10.1080/14756360410001689595.

Abstract

Schiff's bases were obtained from aromatic/heterocyclic sulfonamides and amino-sulfonamide derivatives, such as sulfanilamide, homosulfanilamide, 4-aminoethyl-benzenesulfonamide and 5-amino-1,3,4-thiadiazole-2-sulfonamide. Metal complexes of some of these Schiff's bases, incorporating Zn(II), Co(lI), Ni(II) and Cu(II) ions, were also prepared and tested as inhibitors of the zinc enzyme carbonic anhydrase (CA), and more specifically the red blood cell isozymes I and II. The Schiff's bases behaved as medium potency CA I and CA II inhibitors, whereas their metal complexes showed a highly enhanced potency, with several low nanomolar CA II inhibitors detected.

摘要

席夫碱由芳香族/杂环磺酰胺和氨基磺酰胺衍生物制得,如磺胺、同型磺胺、4-氨基乙基苯磺酰胺和5-氨基-1,3,4-噻二唑-2-磺酰胺。还制备了其中一些席夫碱与锌(II)、钴(II)、镍(II)和铜(II)离子形成的金属配合物,并作为锌酶碳酸酐酶(CA),更具体地说是红细胞同工酶I和II的抑制剂进行了测试。席夫碱表现为中等效力的CA I和CA II抑制剂,而它们的金属配合物显示出效力大幅增强,检测到几种低纳摩尔的CA II抑制剂。

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