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Synthesis of novel tetra‐substituted benzimidazole compounds containing certain heterostructures with antioxidant and anti‐urease activities
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-02-14 , DOI: 10.1002/jhet.3905
Nesrin Karaali 1 , Serdar Aydin 1 , Nimet Baltas 1 , Emre Mentese 1
Affiliation  

A new series of 5,6‐dimethyl‐2‐phenyl‐1H‐benzimidazole derivatives was synthesized. The antioxidant activities of the synthesized compounds were determined according to the cupric reducing antioxidant capacity (CUPRAC), ABTS, and DPPH assays. Many of the target compounds showed good antioxidant activity. Among these compounds, it has been determined that the carbothioamide and 1,2,4‐triazole derivatives had a very good antioxidant capacity. Also, all compounds were screened for in vitro inhibitory activity against Jack bean urease. Among the synthesized molecules, the starting compound, acetate, and acetohydrazide derivatives (with IC50 values 12.02, 11.40, and 8.04 μg/mL, respectively) had a higher inhibitory effect on urease and exhibited a lower IC50 values than acetohydroxamic acid (IC50: 20.50 μg/mL) and thiourea (IC50: 14.04 μg/mL) as a reference inhibitors.

中文翻译:

具有某些具有抗氧化和抗脲酶活性的异质结构的新型四取代苯并咪唑化合物的合成

合成了一系列新的5,6-二甲基-2-苯基-1 H-苯并咪唑衍生物。合成的化合物的抗氧化活性根据铜还原抗氧化能力(CUPRAC),ABTS和DPPH测定法确定。许多目标化合物显示出良好的抗氧化活性。在这些化合物中,已确定碳硫代酰胺和1,2,4-三唑衍生物具有非常好的抗氧化能力。同样,针对所有对波克豆脲酶的抑制活性筛选所有化合物。在合成的分子中,起始化合物,乙酸盐和乙酰肼衍生物(IC 50分别为12.02、11.40和8.04μg/ mL)对脲酶的抑制作用较高,而IC 50较低。比乙酰氧肟酸(IC 50:20.50μg/ mL)和硫脲(IC 50:14.04μg/ mL)更强。
更新日期:2020-02-14
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