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New Conjugates of Quinoxaline as Potent Antitubercular and Antibacterial Agents
Author(s) -
Ramalingam Peraman,
K. Rajendran,
Sunil Kumar Killi,
Y. Padmanabha Reddy
Publication year - 2016
Publication title -
international journal of medicinal chemistry
Language(s) - English
Resource type - Journals
eISSN - 2090-2069
pISSN - 2090-2077
DOI - 10.1155/2016/6471352
Subject(s) - quinoxaline , dna gyrase , chemistry , conjugate , moiety , minimum inhibitory concentration , combinatorial chemistry , stereochemistry , docking (animal) , antibacterial activity , biochemistry , bacteria , in vitro , escherichia coli , biology , organic chemistry , medicine , mathematical analysis , mathematics , nursing , gene , genetics
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  μ 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.

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