Diaryl Azo Derivatives As Anti-diabetic and Antimicrobial Agents: Synthesis, , Kinetic and Docking Studies

Overview

Journal J Enzyme Inhib Med Chem

Specialty Biochemistry

Date 2021 Jul 9

PMID 34238110

Citations 4

Authors

Tehreem Tahir

Mirza Imran Shahzad

Rukhsana Tabassum

Muhammad Rafiq

Muhammad Ashfaq

Mubashir Hassan

Katarzyna Kotwica-Mojzych

Mariusz Mojzych

Affiliations

Soon will be listed here.

Abstract

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.

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