Synthesis and Biological Evaluation of Quinazolonethiazoles as New Potential Conquerors towards Pseudomonas Aeruginosa

Main observation and conclusion Novel quinazolonthiazoles were designed and synthesized as new potential antimicrobial agents by facile multi‐step procedure from o‐aminobenzoic acids and 2‐acetylthiazole. A series of biological evaluation showed that compound 7d was the most effective quinazolonethiazole with superior activity to reference drugs chloramphenicol and norfloxacin. This active molecule displayed unobvious bacterial resistance against P. aeruginosa, the low toxicity to normal hepatocytes, suitable pharmacokinetics and drug‐likeness. The preliminary biological interaction suggested that quinazolonethiazole 7d might induce bacterial death by disturbing the membrane permeability, whilst preventing bacteria from growth by integrating into DNA and binding with topoisomerase IV. These findings provided significant background for the further development of quinazolonethiazoles as new potential drugs in combating drug‐resistant pathogens. A novel class of potential antimicrobial quiazolonethiazoles were developed by multistep synthetic process and their biological evaluation suggested that quiazolonethiazoles could provide the meritorious groundwork of future studies as new antimicrobial agents in fighting pathogenic organism.