In the present study, a series of azo derivatives ( to ) 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 (gram-negative), (gram-positive), (gram-positive) drug-resistant strain, (gram-negative), (gram-negative) drug-resistant strain and (gram-negative). The IC (µg/mL) of was found to be most effective (15.70 ± 1.3 µg/mL) compared to the reference drug acarbose (21.59 ± 1.5 µg/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 () 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.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8274517PMC
http://dx.doi.org/10.1080/14756366.2021.1929949DOI Listing

Publication Analysis

Top Keywords

azo derivatives
8
drug-resistant strain
8
strain gram-negative
8
diaryl azo
4
derivatives anti-diabetic
4
anti-diabetic antimicrobial
4
antimicrobial agents
4
agents synthesis
4
synthesis kinetic
4
kinetic docking
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!