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Efficient Synthesis of 2-[(3,4-Dichlorophenyl)methyl]-1H-benzimidazole Derivatives, and their α-Glucosidase Inhibitory and Antioxidant Activities
Letters in Organic Chemistry ( IF 0.7 ) Pub Date : 2020-09-30 , DOI: 10.2174/1570178617666200330130024
Emre Menteşe 1 , Fatih Yılmaz 2 , Nimet Baltaş 1
Affiliation  

In this work, some new 2-[(3,4-dichlorophenyl)methyl]-1H-benzimidazole derivatives containing different five-membered heterocycles like 1,3,4-oxadiazole, 1,3,4-triazole, and 1,3,4- thiadiazole moieties were designed and efficiently synthesized starting from 2-[(3,4-dichlorophenyl) methyl]-1H-benzimidazole. The products were screened for their in vitro antioxidant and α-glucosidase inhibitory activities. Among the synthesized compounds, some of them showed efficient α-glucosidase inhibition with IC50 values ranging between 16.05 ± 0.94 and 77.02 ± 1.12 μg/mL when they were compared with the standard α-glucosidase inhibitor acarbose having IC50 value 12.04 ± 0.68 μg/mL. The antioxidant activity of all products was screened by using various in vitro antioxidant assays, including CUPric Reducing Antioxidant Capacity (CUPRAC) and Ferric Reducing Antioxidant Power (FRAP) assays. Also, the radical scavenging activities of the products were assayed by using the ABTS method.



中文翻译:

2-[((3,4-二氯苯基)甲基] -1H-苯并咪唑衍生物的合成及其对α-葡萄糖苷酶的抑制和抗氧化活性

在这项工作中,一些新的2-[((3,4-二氯苯基)甲基] -1H-苯并咪唑衍生物包含不同的五元杂环,如1,3,4-恶二唑,1,3,4-三唑和1,3从2-[((3,4-二氯苯基)甲基] -1H-苯并咪唑开始,设计并有效合成了4-4-噻二唑部分。筛选产物的体外抗氧化剂和α-葡萄糖苷酶抑制活性。在合成的化合物中,当与具有IC 50的标准α-葡萄糖苷酶抑制剂阿卡波糖进行比较时,其中一些化合物表现出有效的α-葡萄糖苷酶抑制作用,IC 50值在16.05±0.94和77.02±1.12μg/ mL之间。值12.04±0.68μg/ mL。通过使用各种体外抗氧化剂测定法筛选所有产品的抗氧化活性,包括CUPric还原抗氧化能力(CUPRAC)和铁还原抗氧化能力(FRAP)测定。另外,通过使用ABTS方法测定产物的自由基清除活性。

更新日期:2020-11-18
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