A series of novel calix[4]azacrown substituted sulphonamide Schiff bases was synthesised by the reaction of calix[4]azacrown aldehydes with different substituted primary and secondary sulphonamides. The obtained novel compounds were investigated as inhibitors of six human (h) isoforms of carbonic anhydrases (CA, EC 4.2.1.1). Their antioxidant profile was assayed by various bioanalytical methods. The calix[4]azacrown substituted sulphonamide Schiff bases were also investigated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase enzymes, associated with several diseases such as Alzheimer, Parkinson, and pigmentation disorders. The new sulphonamides showed low to moderate inhibition against hCAs, AChE, BChE, and tyrosinase enzymes. However, some of them possessed relevant antioxidant activity, comparable with standard antioxidants used in the study.

中文翻译：

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具有抗氧化、乙酰胆碱酯酶、丁酰胆碱酯酶、酪氨酸酶和碳酸酐酶抑制作用的杯[4]氮杂冠取代磺酰胺的合成。


通过杯[4]氮杂冠醛与不同取代的伯磺酰胺和仲磺酰胺的反应合成了一系列新型的杯[4]氮杂冠取代的磺酰胺席夫碱。所获得的新化合物作为六种人 (h) 碳酸酐酶亚型 (CA、EC 4.2.1.1) 的抑制剂进行了研究。通过各种生物分析方法测定了它们的抗氧化特性。还研究了杯[4]氮杂冠取代的磺酰胺希夫碱作为乙酰胆碱酯酶 (AChE)、丁酰胆碱酯酶 (BChE) 和酪氨酸酶的抑制剂，这些酶与阿尔茨海默病、帕金森病和色素沉着障碍等多种疾病有关。新的磺胺类药物对 hCA、AChE、BChE 和酪氨酸酶具有低至中度的抑制作用。然而，其中一些具有相关的抗氧化活性，与研究中使用的标准抗氧化剂相当。