Department of Chemistry, University of Selcuk, Konya, Turkey.
Department of Advanced Material and Nanotechnology, Selcuk University, Konya, Turkey.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):1215-1223. doi: 10.1080/14756366.2020.1765166.
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.
通过 calix[4]azacrown 醛与不同取代的伯胺和仲胺的反应，合成了一系列新型 calix[4]azacrown 取代磺酰胺席夫碱。将得到的新型化合物作为六种人源（h）碳酸酐酶（CA，EC 4.2.1.1）同工酶的抑制剂进行了研究。通过各种生物分析方法评估了它们的抗氧化特性。还研究了 calix[4]azacrown 取代磺酰胺席夫碱对乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）和酪氨酸酶的抑制作用，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。新型磺酰胺类化合物对 hCA、AChE、BChE 和酪氨酸酶表现出低至中等抑制作用。然而，其中一些具有相关的抗氧化活性，可与研究中使用的标准抗氧化剂相媲美。
