【摘 要】
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Main observation and conclusionrnNovel 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 comp
【机 构】
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Institute of Bioorganic & Medicinal Chemistry,Key Laboratory of Luminescence Analysis and Molecular
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Main observation and conclusionrnNovel 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 unob-vious 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 mem-brane permeability,whilst preventing bacteria from growth by integrating into DNA and binding with topoisomerase Ⅳ.These find-ings provided significant background for the further development of quinazolonethiazoles as new potential drugs in combating drug-resistant pathogens.
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