DPPH
阿布茨
化学
苯并咪唑
抗坏血酸
抗氧化剂
淀粉酶
IC50型
有机化学
立体化学
生物化学
酶
体外
食品科学
作者
Akinsola Akande,Uzma Salar,Khalid Mohammed Khan,Sabin Syed,Sherifat A. Aboaba,Sridevi Chigurupati,Abdul Wadood,Muhammad Riaz,Muhammad Taha,Saurabh Bhatia,Kanwal,Shahbaz Shamim,Shahnaz Perveen
出处
期刊:ACS omega
[American Chemical Society]
日期:2021-08-26
卷期号:6 (35): 22726-22739
被引量:14
标识
DOI:10.1021/acsomega.1c03056
摘要
Benzimidazole scaffolds are known to have a diverse range of biological activities and found to be antidiabetic and antioxidant. In this study, a variety of arylated benzimidazoles 1–31 were synthesized. Except for compounds 1, 6, 7, and 8, all are new derivatives. All compounds were screened for α-amylase inhibitory, 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities. In vitro screening results revealed that all molecules demonstrated significant α-amylase inhibition with IC50 values of 1.86 ± 0.08 to 3.16 ± 0.31 μM as compared to standard acarbose (IC50 = 1.46 ± 0.26 μM). However, compounds showed significant ABTS and DPPH radical scavenging potentials with IC50 values in the range of 1.37 ± 0.21 to 4.00 ± 0.10 μM for ABTS and 1.36 ± 0.09 to 3.60 ± 0.20 μM for DPPH radical scavenging activities when compared to ascorbic acid with IC50 values of 0.72 ± 0.21 and 0.73 ± 0.05 μM for ABTS and DPPH radical scavenging potentials, respectively. Structure–activity relationship (SAR) was established after critical analysis of varying substitution effects on α-amylase inhibitory and radical scavenging (ABTS and DPPH) potentials. However, molecular docking was also performed to figure out the active participation of different groups of synthetic molecules during binding with the active pocket of the α-amylase enzyme.
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