Synthesis of isoniazid-1,2,3-triazole conjugates: Antitubercular, antimicrobial evaluation and molecular docking study

JOURNAL OF HETEROCYCLIC CHEMISTRY(2020)

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摘要
In the present study, a series of new isoniazid-1,2,3-triazole conjugates (5a-k) was synthesizedviaclick chemistry approach. The newly synthesized compounds were assessed for theirin vitroantitubercular and antimicrobial activities. The compound5ghas displayed potent antitubercular activity againstMycobacterium tuberculosisH37Rv (Mtb) with MIC value 1.56 mu g/mL. The active compounds were screened for their cytotoxicity profile by MTT assay against RAW 264.7 cell line. The four compounds have shown goodin vitroantimicrobial activities against both antibacterial and antifungal pathogens. A molecular docking study was accomplished to identify the probable mode of action of synthesized derivatives. These compounds have shown excellent binding affinity towardEnoyl-acp reductase(INHA) andDNA gyrase.
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