Journal
SYNTHETIC COMMUNICATIONS
Volume 50, Issue 2, Pages 271-288Publisher
TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2019.1695275
Keywords
Antifungal activity; antioxidant activity; antitubercular activity; dimeric 1; 2; 3-triazoles; molecular docking study
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Funding
- Dr. Babasaheb Ambedkar Marathwada University, Aurangabad
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In search of more potent new antitubercular agents, a library of novel piperazine tethered dimeric 1,2,3-triazoles were designed by assembling 1,2,3-triazoles and piperazine in a single molecular architectural framework. The titled compounds (3a-m) were synthesized by 1,3-dipolar cycloaddition of 1,4-di(prop-2-yn-1-yl)piperazine (1) and various azides (2a-m) using click chemistry approach with good yields. All the synthesized compounds (3a-m) have been screened for their in vitro antitubercular, antifungal and antioxidant activities against their respective strains. Among them, 3b, 3d, and 3i have revealed promising antitubercular activity against Mycobacterium tuberculosis (Mtb) H37Rv with MIC 12.5 mu g/mL. Molecular docking results provided well-clustered solutions to the mode of binding for these molecules into the active site of Mtb enoyl reductase (InhA). In addition to this, most of synthesized compounds were found to have potential antifungal as well as antioxidant activity.
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