化学
体外
阿卡波糖
抗氧化剂
生物信息学
活力测定
立体化学
一氧化氮
淀粉酶
生物化学
DPPH
酶
对接(动物)
有机化学
护理部
基因
医学
作者
Malose J. Mphahlele,Nontokozo M. Magwaza,Sibusiso T. Malindisa,Yee Siew Choong
摘要
Abstract The 2‐aryl‐2,3‐dihydrobenzodiazaborinin‐4(1 H )‐ones (azaborininone) were synthesized as analogues of the 2‐arylquinazoline‐4‐ones and screened through enzymatic assay in vitro for inhibitory effect against α‐glucosidase and α‐amylase activities. These azaborininones exhibited moderate to good inhibitory effect against these enzymes compared to acarbose used as a reference standard. The results are supported by the enzyme‐ligand interactions through kinetics (in vitro) and molecular docking (in silico) studies. The test compounds also exhibited significant antioxidant activity through the 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and nitric oxide (NO) free radical scavenging assays. These azaborininone derivatives exhibited no effect on the viability of the human lung cancer (A549) cell line after 24 hr and were also not toxic towards the Vero cells.
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