Abstract
New 1,2,3-triazoles bearing biphenoloxymethyl and acetanilido moieties (5a-5l) have been synthesized, starting from 4-phenylphenol (1) following click chemistry approach. The synthesized compounds have been thoroughly characterized by their 1H NMR, 13C NMR and HRMS spectral data. These compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv and antimicrobial activity against pathogenic microbia. Among the screened compounds, 5a and 5i have displayed notable antitubercular activity with MIC 25 µg/mL. Compounds 5a, 5b, 5c, 5 g, 5i and 5 l have shown effective inhibition against most of tested pathogens. Molecular docking results of compounds 5a and 5i show the binding modes of the synthesized compounds into the active site of mycobacterial enoyl reductase. The synthesized compounds have also been analyzed for their ADME properties. By considering all these results, the present research work will offer a promising lead series for discovery of emerging potent antitubercular agents.
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