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Biological evaluation the 2‐aryl‐2,3‐dihydrobenzodiazaborinin‐4(1 H )‐ones as potential dual α‐glucosidase and α‐amylase inhibitors with antioxidant properties
Author(s) -
Mphahlele Malose J.,
Magwaza tokozo M.,
Malindisa Sibusiso T.,
Choong Yee Siew
Publication year - 2021
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13893
Subject(s) - dpph , acarbose , chemistry , antioxidant , in vitro , enzyme , docking (animal) , biochemistry , in silico , amylase , stereochemistry , viability assay , nitric oxide , aryl , organic chemistry , medicine , nursing , alkyl , gene
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.