Synthesis and evaluation the antibacterial and antifugal activity of cationic amphiphilic derivatives bearing 1,3,4 -oxadiazole scaffold
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Abstract
Background: Based on the antibacterial effect of cationic amphiphilic derivatives, a 1,3,4-oxadiazole framework was designed and synthesized as the cationic amphiphilic and evaluated for their antibacterial and antifungal efficacy. Objective: Synthesize zwitterionic derivatives containing the 1,3,4-oxadiazole scaffold and test the antibacterial and antifungal activity of the synthesized compounds. Subject and method: The zwitterionic 1,3,4-oxadiazole derivatives were synthesized from 4-hydroxybenzaldehyde to form 4-alkoxybenzaldehyde via the Williamson reaction. The oxadiazole heterocycle was synthesized through condensation and redox reactions, followed by amidation with N-Boc amino acids and subsequent deprotection of the -Boc group to obtain the zwitterionic compounds. The structures were determined by 1H-NMR and 13C-NMR. For testing antibacterial and antifungal activities: Microdilution method in liquid medium using broth on a 96-well plate. Result: Six zwitterionic derivatives containing the 1,3,4-oxadiazole scaffold were successfully synthesized; The six synthesized substances did not show activity on the tested strains under concentration of 128µg/mL. Conclusion: The synthesized 1,3,4-oxadiazole derivatives show non-antibacterial and non-antifungal activity on the investigated strain under 128µg/ml concentration. It is necessary to continue researching the synthesis of the more novel derivatives and evaluate the effects on new strains of microorganisms.
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