New Conjugates of Quinoxaline as Potent Antitubercular and Antibacterial Agents

Author:

Peraman Ramalingam1ORCID,Kuppusamy Rajendran2,Killi Sunil Kumar3,Reddy Y. Padmanabha1

Affiliation:

1. Raghavendra Institute of Pharmaceutical Education and Research (RIPER), Andhra Pradesh 5215002, India

2. College of Pharmacy, Gulf Medical University, Ajman, UAE

3. Medicinal Chemistry Division, National Institute of Pharmaceutical Education and Research (NIPER), Kolkata 700032, India

Abstract

Considering quinoxaline as a privileged structure for the design of potent intercalating agents, some new sugar conjugates of quinoxaline were synthesized and characterized by IR, 1HNMR, 13C NMR, and mass spectral data. In vitro testing for antitubercular and antimicrobial activities was performed against Mycobacterium tuberculosis H37Rv and some pathogenic bacteria. Results revealed that conjugate containing ribose moiety demonstrated the most promising activity against Mycobacteria and bacteria with minimum inhibitory concentrations (MIC) of 0.65 and 2.07 μM, respectively. Other conjugates from xylose, glucose, and mannose were moderately active whilst disaccharides conjugates were found to be less active. In silico docking analysis of prototype compound revealed that ATP site of DNA gyrase B subunit could be a possible site for inhibitory action of these synthesized compounds.

Publisher

Hindawi Limited

Subject

Drug Discovery,Molecular Medicine,Biochemistry

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