Development of new drugs with antibacterial potency is an important solution to overcome drug-resistance problems. In the goal to develop novel structure with antibacterial potency, we designed and synthesized novel acridone derivatives bearing triazole nucleus. The novel synthesized compounds were tested for their in vitro antibacterial activity against four bacterial human pathogenic strains. The compound 4h displayed significant antibacterial activities against Staphylcoccus aureus (MRSA) with MIC = 19.6 μg/mL. The synthesized compounds were subjected for docking study to understand the interaction of our compounds and the dihydropteroate synthase (DHPS) in methicillin-resistant Staphylcoccus aureus (MRSA).

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新系列吖啶酮-1,2,3-三唑衍生物的合成、抗菌评价及分子对接研究

开发具有抗菌效力的新药是克服耐药性问题的重要途径。为了开发具有抗菌效力的新型结构，我们设计并合成了带有三唑核的新型吖啶酮衍生物。测试了新合成的化合物对四种细菌人类致病菌株的体外抗菌活性。化合物 4h 对金黄色葡萄球菌 (MRSA) 表现出显着的抗菌活性，MIC = 19.6 μg/mL。对合成的化合物进行对接研究，以了解我们的化合物与二氢蝶呤合酶 (DHPS) 在耐甲氧西林金黄色葡萄球菌 (MRSA) 中的相互作用。