Abstract

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.

摘要

通过杯[4]氮杂卓醛与不同的取代伯，仲磺酰胺反应，合成了一系列新颖的杯[4]氮杂卓取代的磺酰胺席夫碱。研究了所得的新型化合物作为六种人（h）碳酸酐酶同工型的抑制剂（CA，EC 4.2.1.1）。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]氮杂酰胺取代的磺酰胺席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，与多种疾病如阿尔茨海默病，帕金森病和色素沉着症有关。新的磺酰胺类药物显示出对hCAs，AChE，BChE和酪氨酸酶的低至中度抑制作用。但是，其中一些具有相关的抗氧化活性，