Synthesis, Characterization, and Bioactivity Investigation of Novel Benzimidazole Derivatives as Potential Antibacterial and Antifungal Agents
Said Alghawi, Nallusamy Sivakumar, Sedky H. A. Hassan, Raid J. Abdel-Jalil
TL;DR
This study creates and tests new benzimidazole compounds that show promise as antibacterial and antifungal agents.
Contribution
The paper introduces novel benzimidazole derivatives with demonstrated antimicrobial activity and a potential bactericidal mechanism.
Findings
Compound 6h showed the best antibacterial activity with an MIC of 5.0 µg/mL.
SEM analysis revealed that 6h caused cell deformation and membrane disruption in bacteria.
Most compounds displayed moderate to good antimicrobial activity against tested pathogens.
Abstract
A series of benzimidazole derivatives 6a–j was designed and synthesized via the condensation of the corresponding o-phenylenediamine intermediates with formic acid. Antibacterial activity was evaluated in vitro using the agar well diffusion method against Staphylococcus aureus, Bacillus cereus, Escherichia coli, and Klebsiella pneumoniae, with nitrofurantoin (300 µg/mL) as the positive control. Antifungal screening was performed against Aspergillus flavus, Penicillium duclauxii, and P. italicum at 20 and 50 µg/mL, with Amphotericin B as the reference drug at the same concentrations. Most compounds exhibited moderate to good antimicrobial activity. MIC determination identified 6h as the most active antibacterial agent (MIC = 5.0 µg/mL). The SEM analysis of bacteria treated with 6h revealed marked morphological damage, including cell deformation and membrane disruption, supporting a…
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Taxonomy
TopicsSynthesis and biological activity · Multicomponent Synthesis of Heterocycles · Synthesis of Tetrazole Derivatives