Diaryl azo derivatives as anti-diabetic and antimicrobial agents: synthesis, <i>in vitro</i>, kinetic and docking studies
نویسندگان
چکیده
In the present study, a series of azo derivatives (TR-1 to TR-9) have been synthesised via 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), (gram-positive) drug-resistant strain, P. aeruginosa (gram-negative) strain vulgaris (gram-negative). IC50 (µg/mL) TR-1 was found be most effective (15.70 ± 1.3 µg/mL) compared reference drug acarbose (21.59 1.5 µg/mL), hence, it further selected kinetic studies in order illustrate mechanism inhibition. enzyme inhibitory kinetics mode binding active inhibitor (TR-1) performed which showed that compound is non-competitive effectively inhibits target by its binuclear site reversibly.
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2021
ISSN: ['1475-6374', '1475-6366']
DOI: https://doi.org/10.1080/14756366.2021.1929949