Faculty of Education, Department of Science and Mathematics Education, Ondokuz Mayis University, Samsun, Türkiye.
Faculty of Agriculture, Department of Agricultural Biotechnology, Ondokuz Mayıs University, Samsun, Türkiye.
J Enzyme Inhib Med Chem. 2023 Dec;38(1):2194573. doi: 10.1080/14756366.2023.2194573.
A series of sulfenimide derivatives (1a-i) were investigated as inhibitors of human (hCA-I, hCA-II) and bovine (bCA) carbonic anhydrase enzymes. The compounds were synthesised by the reaction of substituted thiophenols with phthalimide by means of an effective, simple and eco-friendly method and the structures were confirmed by IR, H NMR, C NMR, MS and elemental analysis. All derivatives except for the methyl derivative () exhibited effective inhibitory action at low micromolar concentrations on human isoforms, but only four derivatives (, , , ) inhibited the bovine enzyme. The bromo derivative ( was found to be strongest inhibitor of all three enzymes with KI values of 0.023, 0.044 and 20.57 µM for hCA-I, hCA-II and bCA, respectively. Results of our study will make valuable contributions to carbonic anhydrase inhibition studies for further investigations since inhibitors of this enzyme are important molecules for medicinal chemistry.
研究了一系列亚磺酰亚胺衍生物（1a-i）作为人（hCA-I、hCA-II）和牛（bCA）碳酸酐酶抑制剂。这些化合物是通过取代的噻酚与邻苯二甲酰亚胺反应，采用有效、简单和环保的方法合成的，其结构通过 IR、H NMR、C NMR、MS 和元素分析得到确认。除了甲基衍生物（）之外，所有衍生物在低微摩尔浓度下对人同工酶均表现出有效的抑制作用，但只有 4 种衍生物（、、、）抑制牛酶。溴代衍生物（对三种酶的抑制作用最强，KI 值分别为 0.023、0.044 和 20.57µM。我们的研究结果将为碳酸酐酶抑制研究做出有价值的贡献，因为该酶的抑制剂是药物化学中重要的分子。
