ABSTRACT
AIM: To investigate a novel series of quinazoline monopeptide esters for the in vitro antibacterial activity. METHODOLOGY/RESULTS: The compounds were synthesized via one-pot Dimroth rearrangement of suitable formamidine intermediates with 3-aminobenzoic acid, followed by coupling the resulting acids with amino acid esters and screening for their antibacterial activity by broth dilution method. The compounds 5a, 5b, 5c, 5g, 5i and 5j showed promising activity against the Gram-positive bacteria, 5c and 5g being the most potent against Enterococcus faecalis and Staphylococcus aureus, respectively, with a minimal inhibitory concentration of 0.51 µM. The percentage hemolysis of the compounds ranged from 2.79 to 12.92 at a concentration of 100 µg/ml. The molecular docking studies revealed their GlmU inhibitory action. CONCLUSION: The compounds 5a and 5g emerged as antibacterial hits.
