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

In the present study, a series of new isoniazid‐1,2,3‐triazole conjugates (5a‐k) was synthesized via click chemistry approach. The newly synthesized compounds were assessed for their in vitro antitubercular and antimicrobial activities. The compound 5g has displayed potent antitubercular activity ag...

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Published in:Journal of heterocyclic chemistry 2020-10, Vol.57 (10), p.3544-3557
Main Authors: Badar, Adinath D., Sulakhe, Shubham M., Muluk, Mahesh B., Rehman, Naziya N. M. A., Dixit, Prashant P., Choudhari, Prafulla B., Rekha, Estharla Madhu, Sriram, Dharmarajan, Haval, Kishan P.
Format: Article
Language:English
Subjects:
Chemical synthesis
Conjugates
Fungicides
Molecular docking
Reductases
Toxicity
Triazoles
Tuberculosis
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Summary:In the present study, a series of new isoniazid‐1,2,3‐triazole conjugates (5a‐k) was synthesized via click chemistry approach. The newly synthesized compounds were assessed for their in vitro antitubercular and antimicrobial activities. The compound 5g has displayed potent antitubercular activity against Mycobacterium tuberculosis H37Rv (Mtb) with MIC value 1.56 μg/mL. The active compounds were screened for their cytotoxicity profile by MTT assay against RAW 264.7 cell line. The four compounds have shown good in vitro antimicrobial 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 toward Enoyl‐acp reductase (INHA) and DNA gyrase.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.4072