化学
DPPH
苯并呋喃
抗氧化剂
阿布茨
有机化学
IC50型
立体化学
核化学
体外
药物化学
生物化学
作者
Irfan Ali,Rafaila Rafique,Mohammed M. Alanazi,Sridevi Chigurupati,Xingyue Ji,Abdul Wadood,Ashfaq Ur Rehman,Uzma Salar,Muhammad Shahid Iqbal,Muhammad Taha,Shahnaz Perveen,Basharat Ali
标识
DOI:10.1016/j.bioorg.2020.104238
摘要
Thirty benzofuran-2-yl(phenyl)methanones 1–30 were synthesized and characterized their structures by spectroscopic techniques. Substituted phenacyl bromide and different derivatives of 2-hydroxy-benzaldehyde treated in the presence of anhydrous K2CO3 in acetonitrile at room temperature to afford the desired benzofurans 1–30. All compounds were screened for their in vitro α-amylase inhibitory and radical scavenging (DPPH and ABTS) activities. Results revealed that para substituted compounds were found to be more active than the others with IC50 values ranges for α-amylase inhibition (IC50 = 18.04–48.33 µM), DPPH (IC50 = 16.04–32.33 µM) and ABTS (IC50 = 16.99–33.01 µM) radical scavenging activities. Activities results were compared with the standards acarbose (IC50 = 16.08 ± 0.07 µM) for α-amylase, ascorbic acid (IC50 = 15.08 ± 0.03 and 15.09 ± 0.17 µM) for DPPH and ABTS radical scavenging activities, respectively. Kinetic studies predicted that all compounds followed non-competitive mechanism of inhibition. Molecular docking results showed good protein–ligand interactions profile against the corresponding target. To the best of our knowledge, out of thirty molecules, ten compounds 18–20, 22, and 25–30 were structurally new.
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