首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Sulphonamides incorporating 1,3,5-triazine structural motifs show antioxidant, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory profile
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Sulphonamides incorporating 1,3,5-triazine structural motifs show antioxidant, acetylcholinesterase, butyrylcholinesterase, and tyrosinase inhibitory profile

机译:含有1,3,5-三嗪结构基质的磺胺酰胺显示抗氧化剂,乙酰胆碱酯酶,丁二醇酸酶和酪氨酸酶抑制型材

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摘要

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.
机译:研究了包含由芳族胺,二甲胺,吗啉和哌啶取代的1,3,5-三嗪部分的16种新型苯磺胺酰胺。通过使用1,1-二苯基-2-富铬酰肼(DPPH)自由基清除测定,2,2-αzino-BIS(3-乙基苯并噻唑啉-6-磺酸(ABTS)自由基脱色测定和金属,测定这些化合物进行抗氧化性能螯合方法。还研究它们作为乙酰胆碱酯酶(ACHE),丁二醇酸碱酯酶(BCHE)和酪氨酸酶的抑制剂,其与几种疾病如阿尔茨海默,帕金森和色素沉着病症相关。这些苯并磺胺酰胺显示出中度DPPH激进清除和金属螯合活性,以及低血管阳离子自由基清除活性。化合物2?B,3D和3?H显示出疼痛的抑制作用> 90%的抑制值> 90.大多数合成化合物也有效地抑制了β0%的抑制效力。酪氨酸酶是有效的。酪氨酸酶是有效的。酪氨酸酶是酪氨酸酶这些化合物的抑制较小。

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