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Synthesis, antibacterial evaluation and molecular docking studies of novel series of acridone-1,2,3-triazole derivatives

机译:新型吖啶酮-1,2,3-三唑衍生物新型系列的合成,抗菌评价及分子对接研究

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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 mu g/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).
机译:抗菌效力的新药的发展是克服耐药问题的重要解决方案。 在患有抗菌性效力的新型结构中,我们设计和合成了载有三唑核的新型吖啶酮衍生物的新型结构。 测试新的合成化合物,用于对四种细菌人致病菌株的体外抗菌活性进行测试。 化合物4H用MIC =19.6μg/ mL对含有金黄色葡萄球菌(MRSA)的显着抗菌活性。 进行合成化合物进行对接研究以了解我们的化合物和二氢酯合酶(DHPS)在甲氧西林耐金黄色葡萄球菌(MRSA)的相互作用。

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