Nazarbahjat Nafal, Nordin Nurdiana, Abdullah Zanariah, Abdulla Mahmood Ameen, Yehye Wageeh A, Halim Siti Nadiah Abdul, Kee Chin Hui, Ariffin Azhar
Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur, Malaysia.
Department of Biomedical Science, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia.
Molecules. 2014 Aug 4;19(8):11520-37. doi: 10.3390/molecules190811520.
New thiosemicarbazide derivatives 2-6 were synthesised by reacting 2-(ethylsulfanyl)benzohydrazide with various aryl isothiocyanates. The cyclisation of compounds 2-6 under reflux conditions in a basic medium (aqueous NaOH, 4 N) yielded compounds 7-11 that contain a 1,2,4-triazole ring. All of the synthesised compounds were screened for their antioxidant activities. Compounds 2, 3, and 7 showed better radical scavenging in a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, with IC50 values of 1.08, 0.22, and 0.74 µg/mL, respectively, compared to gallic acid (IC50, 1.2 µg/mL). Compound 3 also showed superior results in a ferric reducing antioxidant power (FRAP) assay (3054 µM/100 g) compared to those of ascorbic acid (1207 µM/100 g).
通过使2-(乙硫基)苯甲酰肼与各种芳基异硫氰酸酯反应合成了新型氨基硫脲衍生物2-6。化合物2-6在碱性介质(4N氢氧化钠水溶液)中回流条件下环化，得到含有1,2,4-三唑环的化合物7-11。对所有合成的化合物进行了抗氧化活性筛选。在2,2-二苯基-1-苦基肼(DPPH)测定中，化合物2、3和7表现出较好的自由基清除能力，IC50值分别为1.08、0.22和0.74μg/mL，而没食子酸的IC50值为1.2μg/mL。与抗坏血酸(1207μM/100g)相比，化合物3在铁还原抗氧化能力(FRAP)测定中也显示出优异的结果(3054μM/100g)。
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