期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 36, 期 1, 页码 1509-1520出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2021.1929949
关键词
Antibacterial; anti-diabetic; azo derivatives; molecular docking; phenolic compounds
A series of azo derivatives were synthesized and evaluated for their therapeutic applications against alpha-glucosidase and pathogenic bacterial strains, with TR-1 showing the most effective inhibition as a non-competitive inhibitor binding reversibly to the enzyme's binuclear active site.
In the present study, a series of azo derivatives (TR-1 to TR-9) have been synthesised via the diazo-coupling approach between substituted aromatic amines with phenol or naphthol derivatives. The compounds were evaluated for their therapeutic applications against alpha-glucosidase (anti-diabetic) and pathogenic bacterial strains E. coli (gram-negative), S. aureus (gram-positive), S. aureus (gram-positive) drug-resistant strain, P. aeruginosa (gram-negative), P. aeruginosa (gram-negative) drug-resistant strain and P. vulgaris (gram-negative). The IC50 (mu g/mL) of TR-1 was found to be most effective (15.70 +/- 1.3 mu g/mL) compared to the reference drug acarbose (21.59 +/- 1.5 mu g/mL), hence, it was further selected for the kinetic studies in order to illustrate the mechanism of inhibition. The enzyme inhibitory kinetics and mode of binding for the most active inhibitor (TR-1) was performed which showed that the compound is a non-competitive inhibitor and effectively inhibits the target enzyme by binding to its binuclear active site reversibly.
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