Biological and Medicinal Chemistry

Antimicrobial activities of hydrazones with a 2,4-dichloro moiety.



The goal of this research was to come up with novel antibacterial agents. Two hydrazones with a 2,4-dichloro moiety were synthesized by conventional synthetic methods with good yields. The success of the synthesis was confirmed by structure determination techniques; FITR and NMR analyses. The synthesized hydrazones were evaluated for antimicrobial activity using strains of bacterial and fungi. The two hydrazones demonstrated significant antibacterial and antifungal activities that were comparable to those of ciprofloxacin and fluconazole, respectively. Specifically, compound 3b with a para nitro group on its aniline fragment indicated a broader spectrum of activity compared to compound 3a. Additionally, the two hydrazones were active against bacterial strains such as Staphylococcus aureus, Campylobacter fetus, Proteus, mirabilis, and methicillin-resistant Staphylococcus aureus, which were resistant to ciprofloxacin with a ZI of between 25-31 mm and MIC of 12.5 μg/ml for Proteus mirabilis and 25 μg/ml for others, accordingly. Amazingly, the two hydrazones demonstrated bactericidal and fungicidal activity between 25 μg/ml and 100 μg/ml against all the sensitive bacterial and fungal strains. The two hydrazones with a 2,4-dichloro moiety have been identified as leads and are recommended for further in-vivo efficacy studies.


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