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New Conjugates of Quinoxaline as Potent Antitubercular and Antibacterial Agents.

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, (1)HNMR, (13)C NMR, and mass spectral data. In vitro testing for antitubercular and antimicrobial activities was performed against Mycobacterium tuberculosis H 37 Rv 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??M, 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.

SUBMITTER: Peraman R

PROVIDER: S-EPMC4802037 | biostudies-literature | 2016

REPOSITORIES: biostudies-literature

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New Conjugates of Quinoxaline as Potent Antitubercular and Antibacterial Agents.

Peraman Ramalingam R Kuppusamy Rajendran R Killi Sunil Kumar SK Reddy Y Padmanabha YP

International journal of medicinal chemistry 20160308

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, (1)HNMR, (13)C NMR, and mass spectral data. In vitro testing for antitubercular and antimicrobial activities was performed against Mycobacterium tuberculosis H 37 Rv and some pathogenic bacteria. Results revealed that conjugate containing ribose moiety demonstrated the most promising activity against Mycobacteria and b ...[more]

PMID: 27051530

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