当前位置: X-MOL 学术J. Enzyme Inhib. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Sulphonamides incorporating 1,3,5-triazine structural motifs show antioxidant, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory profile
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2020-01-03
Nabih Lolak, Mehmet Boga, Muhammed Tuneg, Gulcin Karakoc, Suleyman Akocak, Claudiu T. Supuran

A series of 16 novel benzenesulfonamides incorporating 1,3,5-triazine moieties substituted with aromatic amines, dimethylamine, morpholine and piperidine were investigated. These compounds were assayed for antioxidant properties by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay, 2,2`-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical decolarisation assay and metal chelating methods. They were also investigated as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase, which are associated with several diseases such as Alzheimer, Parkinson and pigmentation disorders. These benzenesulfonamides showed moderate DPPH radical scavenging and metal chelating activity, and low ABTS cation radical scavenging activity. Compounds 2 b, 3d and 3 h showed inhibitory potency against AChE with % inhibition values of >90. BChE was also effectively inhibited by most of the synthesised compounds with >90% inhibition potency. Tyrosinase was less inhibited by these compounds.



中文翻译:

包含1,3,5-三嗪结构基序的磺胺类药物显示抗氧化剂,乙酰胆碱酯酶,丁酰胆碱酯酶和酪氨酸酶抑制谱

研究了一系列16种新颖的1,5,3-三嗪部分被芳族胺,二甲胺,吗啉和哌啶取代的苯磺酰胺。通过使用1,1-二苯基-2-吡啶甲基肼基(DPPH)自由基清除试验,2,2'-叠氮基双(3-乙基苯并噻唑啉-6-磺酸(ABTS)自由基脱碳试验和金属来测定这些化合物的抗氧化性能还研究了它们作为乙酰胆碱酯酶(AChE),丁酰胆碱酯酶(BChE)和酪氨酸酶的抑制剂,它们与多种疾病如阿尔茨海默病,帕金森病和色素沉着症有关,这些苯磺酰胺显示出中等的DPPH自由基清除和金属螯合活性,并且低ABTS阳离子自由基清除活性。化合物2 b3d3小时显示出对AChE的抑制效力,%抑制值> 90。大多数合成的化合物还可以有效抑制BChE,抑制效力> 90%。这些化合物对酪氨酸酶的抑制作用较小。

更新日期:2020-01-04
down
wechat
bug