Development of Novel Anti-Infective and Antioxidant Azole Hybrids using a Wet and Dry Approach

Abstract

Background: Considering emerging drug resistance in microbes, this work is focused on the synthesis of azole hybrids as novel antimicrobials. Materials & methods: The triazole derivatives were prepared using azide alkyne cycloaddition reaction. The antimicrobial potential of these compounds was evaluated by serial dilution method. Results: A series of azole hybrids containing benzimidazole-1,2,3-triazole skeleton was designed and synthesized via click reaction. Compound 4s showed notable antimicrobial activity against Staphylococcus aureus and Candida albicans (MIC 0.0165 μmol/ml), and 4q gives remarkable radical scavenging activity (IC50 0.0092 μmol/ml). The compounds 4a, 4k, 4o, 4s, 4x. 4m, 4n, 4s, 4t and 4x are commendable antibacterial and antifungal molecules, even better than established drugs. Molecular docking reveals that compound 4s binds with tyrosyl-tRNA synthetase residues through two H-bonds. Conclusion: Compounds 4s and 4k may be considered valuable lead compounds for further optimization as antimicrobial drugs.

Transition metal complexes of triazole-based bioactive ligands: synthesis, spectral characterization, antimicrobial, anticancer and molecular docking studies

“…The in-vitro antimicrobial activity of all the synthesized compounds ( 1–20 ) was assessed against four bacterial strains and two fungal strains. Norfloxacin and Fluconazole were used as positive control for bacteria and fungi [ 35 ]. DMSO was used as a negative control.…”

“…The resulting mixture was autoclaved at 15 psi for 30 min. The prepared cultures were incubated at 37 °C for 24 h in case of antibacterial culture and at 27 °C for seven days in case of antifungal culture [ 35 ].…”