The invention relates to a 4,5-glyoxalidine [1,2-a] quinoline derivative shown as the following formula (1) and application of the 4,5- glyoxalidine [1,2-a] quinoline derivative, wherein R represents C1-C12 alkyls, benzyl and substituted benzyl, Y represents H, O and N, and R1 represents C1-C12 alkyls, phenyl, substituted phenyl, benzyl and substituted benzyl. The invention also provides a medicine composition containing the derivative and salts of the derivative, and application of the derivative and the salts of the derivative to antibacterial medicine preparation. The derivative and the salts of the derivative respectively have the inhibition effects on staphylococcus aureus, escherichia coli, other gram-negative bacteria (such as pseudomonas aeruginosa, Klebsiella pneumoniae, proteusbacillus vulgaris, salmonella and pasteurella) and gram-positive bacteria, and in other aspects, the antibacterial effect is better than that of ciprofloxacin and amoxicillin.