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Synthesis, Characterization, Molecular Docking, Cell viability and Biological Activity of New Metronidazole Analogues against Cellulitis Causing Pathogens

Year: 2025

Type: article

Abstract: Development of microbial resistance against commercial imidazoles intended present study to develop some new metronidazole analogues against cellulitis causing pathogens. In present study, N-(4-substituted benzylidene)-2-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-acetohydrazide (2a-c) were synthesized by treating hydrazide derivative of metronidazole (1) with various aromatic aldehydes. The structures of synthesized compounds 2a-c were characterized using FT-IR, 1H NMR, 13C NMR and mass spectrometric data. The synthesized compounds 2a-c were evaluated for their inhibitory potential against cellulitis triggering bacteria S. aureus, E. coli and cell viability profile using MTT assay. Among compounds 2a-c, compound 2c incorporated with high electronegative group, exhibited maximum inhibitory potential against cellulitis triggering pathogens. This potential was also supported by the docking data of compounds 2c against glucosamine-6-phosphate (2VF5). The significant antibacterial potential of compounds 2a-c against S. aureus and E. coli, high cell viability against HEK 293 cells (more than 75%) and high docking score of compounds with 2VF5 supports their potential application in cellulitis treatment. However, the synthesized compounds should be further evaluated for their in vivo preclinical significance.

Source: Asian Journal of Chemistry

DOI: 10.14233/ajchem.2025.33675