首页> 美国卫生研究院文献>Journal of Enzyme Inhibition and Medicinal Chemistry >Synthesis of calix4azacrown substituted sulphonamides with antioxidantacetylcholinesterase butyrylcholinesterase tyrosinase and carbonic anhydrase inhibitoryaction
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Synthesis of calix4azacrown substituted sulphonamides with antioxidantacetylcholinesterase butyrylcholinesterase tyrosinase and carbonic anhydrase inhibitoryaction

机译:用抗氧化剂合成杯4氮杂卓取代的磺酰胺乙酰胆碱酯酶丁酰胆碱酯酶酪氨酸酶和碳酸酐酶抑制行动

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摘要

A series of novel calix[4]azacrown substituted sulphonamide Schiff bases was synthesisedby the reaction of calix[4]azacrown aldehydes with different substituted primary andsecondary sulphonamides. The obtained novel compounds were investigated as inhibitors ofsix human (h) isoforms of carbonic anhydrases (CA, EC 4.2.1.1). Their antioxidant profilewas assayed by various bioanalytical methods. The calix[4]azacrown substitutedsulphonamide Schiff bases were also investigated as inhibitors of acetylcholinesterase(AChE), butyrylcholinesterase (BChE) and tyrosinase enzymes, associated with severaldiseases such as Alzheimer, Parkinson, and pigmentation disorders. The new sulphonamidesshowed low to moderate inhibition against hCAs, AChE, BChE, and tyrosinase enzymes.However, some of them possessed relevant antioxidant activity, comparable with standardantioxidants used in the study.
机译:合成了一系列新颖的杯[4]氮杂卓取代的磺酰胺席夫碱杯[4]氮杂row醛与不同取代伯和仲磺酰胺。研究了获得的新型化合物作为缓蚀剂的抑制剂碳酸酐酶的六种人(h)同工型(CA,EC 4.2.1.1)。他们的抗氧化特性通过各种生物分析方法进行了测定。杯[4] azacrown替代还研究了磺酰胺席夫碱作为乙酰胆碱酯酶的抑制剂(AChE),丁酰胆碱酯酶(BChE)和酪氨酸酶,与几种老年痴呆症,帕金森症和色素沉着症等疾病。新的磺酰胺对hCAs,AChE,BChE和酪氨酸酶显示出低至中度的抑制作用。但是,其中一些具有相关的抗氧化活性,与标准品相当研究中使用的抗氧化剂。

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