A novel series of quinolone-based heterocyclic derivatives including thiadiazine, thiadiazoles, and triazole were synthesized and their in vitro antibacterial activity against Gram-positive and Gram-negative bacteria were evaluated. Newly synthesized derivatives have been obtained in good yields ranging from 65 to 80%. The synthesized derivatives have been characterized and their structures identified using spectroscopic analysis including NMR, FT-IR, and mass techniques. Most of compounds exhibited moderate-to-good antibacterial activity against all four bacterial strains and are significantly more active than ampicillin. Compounds showed relatively good anti-bacterial activity compared to moderate activity of other compounds. The results obtained herein are important for further structure modifications of quinoline bearing heterocyclic moiety and the exploitation of the therapeutic potential of quinoline derivatives as antibacterial agents.

Graphic abstract

中文翻译：

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新的基于喹啉的杂环衍生物作为新型抗菌剂的设计，合成和生物学评估

合成了一系列新的基于喹诺酮的杂环衍生物，包括噻二嗪，噻二唑和三唑，并评估了它们对革兰氏阳性和革兰氏阴性细菌的体外抗菌活性。以65％至80％的高产率获得了新合成的衍生物。已对合成的衍生物进行了表征，并使用包括NMR，FT-IR和质谱技术在内的光谱分析鉴定了其结构。大多数化合物对所有四种细菌菌株均表现出中等至良好的抗菌活性，并且比氨苄西林具有明显更高的活性。与其他化合物的中等活性相比，这些化合物显示出相对较好的抗菌活性。

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