Synthesis and characterisation of novel 4,6-dimethoxyindole-7- and -2-thiosemicarbazone derivatives: Biological evaluation as antioxidant and anticholinesterase candidates
Synthesis and characterisation of novel 4,6-dimethoxyindole-7- and -2-thiosemicarbazone derivatives: Biological evaluation as antioxidant and anticholinesterase candidates
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新型 4,6-二甲氧基吲哚-7-和-2-缩氨基硫脲衍生物的合成和表征：作为抗氧化剂和抗胆碱酯酶候选物的生物学评价
DOI：
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发表时间：
2019
期刊：
影响因子：
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通讯作者：
Murat Bingül
中科院分区：
文献类型：
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作者：
Murat Bingül
由吲哚甲醛4和6与一系列缩氨基硫脲7a-d进行席夫碱缩合反应，高产率、高纯度地合成了两组新型吲哚缩氨基硫脲8a-d和9a-d。采用3种不同的方法测定了化合物8a-d和9a-d的抗氧化性能，即清除2，2-二苯基-1-苦基肼自由基、阳离子自由基脱色和铜离子还原抗氧化能力。通过乙酰胆碱酯酶和丁酰胆碱酯酶抑制试验考察了产物的抗胆碱酯酶性能。甲基取代化合物8b和9b对ABTS测定的抑制率和铜离子还原抗氧化能力测定的吸光度最高，而化合物9c对2，2-二苯基-1-苦基肼的测定显示出最好的活性。在化合物8b的情况下，确定了乙酰胆碱酯酶和丁酰胆碱酯酶的适度抑制。
Two sets of novel indole-based thiosemicarbazone systems 8a–d and 9a–d are prepared by the Schiff base condensation reaction of indole carbaldehydes 4 and 6 with a range of thiosemicarbazides 7a–d in high yields and purity. The antioxidant properties of the synthesised compounds 8a–d and 9a–d are determined by employing three different assays, namely 2,2-diphenyl-1-picrylhydrazyl hydrate–free radical scavenging, ABTS [2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)] cationic radical decolarization and cupric ion reducing antioxidant capacity. The anticholinesterase properties of the products are investigated by acetylcholinesterase and butyrylcholinesterase enzyme inhibition assays. The methyl-substituted compounds 8b and 9b display the highest inhibition for the ABTS assay and absorbance values for the cupric ion reducing antioxidant capacity assay, while compound 9c shows the best activity for 2,2-diphenyl-1-picrylhydrazyl hydrate assay. Moderate inhibition of acetylcholinesterase and butyrylcholinesterase is determined in the case of compound 8b.
影响因子：
3.5
作者：
Macdonough MT;Strecker TE;Hamel E;Hall JJ;Chaplin DJ;Trawick ML;Pinney KG
通讯作者：
Pinney KG