Development of new antimicrobial agents is a good solution to overcome drug-resistance problems. From this perspective, new quinoxaline derivatives bearing various bioactive heterocyclic moieties (thiadiazoles, oxadiazoles, pyrazoles and thiazoles) were designed and synthesized. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against nine bacterial human pathogenic strains using the disc diffusion assay. In general, most of the synthesized compounds exhibited good antibacterial activities. The thiazolyl 11c displayed significant antibacterial activities against P. aeruginosa (MIC, 12.5 µg/mL vs levofloxacin 12.5 µg/mL). Molecular docking studies indicated that the synthesized compounds could occupy both p-amino benzoic acid (PABA) and pterin binding pockets of the dihydropteroate synthase (DHPS), suggesting that the target compounds could act by the inhibition of bacterial DHPS enzyme. The results provide important information for the future design of more potent antibacterial agents.

开发新的抗菌剂是克服耐药性问题的一个很好的解决方案。从这个角度出发，设计并合成了具有各种生物活性杂环部分（噻二唑，恶二唑，吡唑和噻唑）的新喹喔啉衍生物。使用盘扩散测定法评估了新合成的化合物对九种细菌人致病菌株的体外抗菌活性。通常，大多数合成化合物表现出良好的抗菌活性。噻唑基11c对铜绿假单胞菌显示出显着的抗菌活性（MIC为12.5 µg / mL，而左氧氟沙星为12.5 µg / mL）。分子对接研究表明，合成的化合物可以占据两个p-二氢蝶呤合酶（DHPS）的β-氨基苯甲酸（PABA）和蝶呤结合口袋，表明目标化合物可以通过抑制细菌DHPS酶发挥作用。结果为将来设计更有效的抗菌剂提供了重要的信息。