Synthesis of isoniazid‐1, 2, 3‐triazole conjugates: Antitubercular, antimicrobial evaluation and molecular docking study. (5th August 2020)

• Record Type: Journal Article
• 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.
• Is Part Of: Journal of heterocyclic chemistry. Volume 57:Number 10(2020)
• Page Start: 3544
• Page End: 3557
• Publication Date: 2020-08-05
• Subjects: Heterocyclic compounds -- Periodicals; 547.59
• DOI: 10.1002/jhet.4072
• Languages: English
• ISSNs: 0022-152X

Abstract

Abstract: 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 . Abstract :