Antibacterial activity of the structurally novel ocotillol-type lactone and its analogues.

A novel series of ocotillol-type lactone derivatives were designed and synthesized in order to study their antibacterial activity and structure-activity relationships. Among which, compounds 4j and 4 m were found to be the most active with minimum inhibitory concentrations (MICs) of 1-4 μg/mL against Gram-positive bacteria and showed low cytotoxicity against MCF-7, HEK-293 and HK-2 cells at their MICs. The antibacterial effect of compound 4 m was characterized further by scanning electron microscopy, cytoplasmic β-galactosidase leakage assay and UV-visible analysis. The results showed that 4 m may exert its antibacterial effect by damaging bacterial cell membranes and disrupting the function of DNA, both of which could lead to rapid cell death.