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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Inhibition of carbonic anhydrase isoforms I, II, IX and XII with Schiff’s bases incorporating iminoureido moieties
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Inhibition of carbonic anhydrase isoforms I, II, IX and XII with Schiff’s bases incorporating iminoureido moieties

机译：带有亚氨基脲基的席夫碱对碳酸酐酶同工型I，II，IX和XII的抑制作用

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摘要

A series of new Schiff’s bases was obtained from the sulfanilamide semicarbazone (4-aminosulfonylphenyl semicarbazide) and aromatic/heterocyclic aldehydes. The new compounds were designed to incorporate moieties known to induce effective inhibitory activity against carbonic anhydrase (CA, EC 4.2.1.1) isoforms involved in crucial physiologic or pathologic processes such as the cytosolic CA I and II or the transmembrane, tumor-associated CA IX and XII: the compounds were medium potency – weak CA I inhibitors, highly effective, low nanomolar CA II inhibitors, but few of them inhibited effectively CA IX and XII. This may probably due to the long spacer between the sulfamoylphenyl and imine fragments of the molecules, which probably induces a highly flexible conformation of the inhibitor bound to the active site of the enzyme, with destabilizing effects for the adduct. The detailed structure activity relationship for this class of inhibitors is discussed.
机译：从磺胺半脲（4-氨基磺酰基苯基氨基脲）和芳香族/杂环醛中获得了一系列新的席夫碱。这些新化合物的设计目的是结合已知能诱导对碳酸酐酶（CA，EC 4.2.1.1）同工型有效抑制活性的部分，这些同工型涉及关键的生理或病理过程，例如胞质CA I和II或跨膜，与肿瘤相关的CA IX和XII：该化合物具有中等效力-弱CA I抑制剂，高效，低纳摩尔CA II抑制剂，但很少有人能有效抑制CA IX和XII。这可能是由于氨磺酰基苯基和分子的亚胺片段之间的长间隔基，这可能诱导与酶的活性位点结合的抑制剂的高度柔性构象，并对加合物产生不稳定作用。讨论了这类抑制剂的详细结构活性关系。

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