Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Adiyaman University, Adiyaman, Turkey.
Department of Analytical Chemistry, Faculty of Pharmacy, Dicle University, Diyarbakir, Turkey.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):424-431. doi: 10.1080/14756366.2019.1707196.
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 , and 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.
研究了一系列 16 种新型苯磺酰胺，其中包含取代芳香胺、二甲胺、吗啉和哌啶的三嗪部分。这些化合物通过使用 1,1-二苯基-2-苦基肼（DPPH）自由基清除测定法、2,2`-联氮双（3-乙基苯并噻唑啉-6-磺酸）（ABTS）自由基脱色测定法和金属螯合方法来测定其抗氧化性能。它们还被研究为乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）和酪氨酸酶的抑制剂，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。这些苯磺酰胺表现出中等的 DPPH 自由基清除和金属螯合活性，以及低的 ABTS 阳离子自由基清除活性。化合物 、 和 对 AChE 表现出抑制活性，抑制率值>90%。大多数合成化合物对 BChE 也有有效的抑制作用，抑制率>90%。这些化合物对酪氨酸酶的抑制作用较小。
