Synthesise and test antibacterial activities of 1,3-benzodioxole derivatives

Novel chemical entities are urgently needed to develop new antibacterial agents in order to tackle the increasing antibiotic resistance. This study focuses on the 1,3-benzodioxole scaffold with promising biological activities in the literature. Five 1,3-benzodioxole containing derivatives were synthesised from piperonal as starting material by various chemical reactions. Their structures were elucidated by standard spectroscopic methods. The in vitro antibacterial activities were studied by agar diffusion method against 5 pathogenic strains: Escherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis, methicillin-susceptible Staphylococcus aureus(MSSA), and methicillin-resistant Staphylococcus aureus (MRSA). The Schiff base derivative (2) showed the ability to inhibit 4/5 tested strains, including MRSA. The target prediction study suggested the in silico binding ability of (2) on the bacterial FabH enzyme. These results demonstrated that novel 1,3-benzodioxole derivatives containing Schiff bases could be further studied as new antibacterial structures.