Rastkari Noushin, Abdollahi Mohammad, Ahmadkhaniha Reza, Shafiee Abbas
Center for Environmental Research, Tehran University of Medical Sciences, Tehran, Iran.
Arch Pharm (Weinheim). 2008 Jan;341(1):49-54. doi: 10.1002/ardp.200700099.
Substituted benzimidazolo[2,1-b]benzo[e]thiazepin-5(10H)-one derivatives were prepared in moderate to good yield by reaction of mercapto benzimidazole derivatives with 2-chloromethylbenzoyl chloride as a coupling component. Their structures were confirmed by elemental analysis, IR, NMR, and MS. Their antioxidant properties were evaluated by several methods: scavenging effect on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals, reducing power assay, and inhibition of lipid peroxidation. In DPPH assay, 3h exhibited an activity stronger than trolox. In the reducing power assay and inhibition of lipid peroxidation, compound 3a was more active than 3h and similar to trolox. The antidiabetic effect was also determined, and the antidiabetic activities were correlated with their antioxidant properties, compound 3a was the most active compound in the in-vivo experiments.
通过巯基苯并咪唑衍生物与2-氯甲基苯甲酰氯作为偶联组分反应，以中等至良好的产率制备了取代的苯并咪唑并[2,1-b]苯并[e]硫氮杂䓬-5(10H)-酮衍生物。通过元素分析、红外光谱、核磁共振和质谱对其结构进行了确证。通过多种方法对其抗氧化性能进行了评估：对1,1-二苯基-2-苦基肼基（DPPH）自由基的清除作用、还原力测定以及脂质过氧化抑制。在DPPH测定中，3h表现出比曲洛昔芬更强的活性。在还原力测定和脂质过氧化抑制中，化合物3a比3h更具活性且与曲洛昔芬相似。还测定了其抗糖尿病作用，并且抗糖尿病活性与它们的抗氧化性能相关，化合物3a是体内实验中活性最高的化合物。
