Levofloxacin hydrochloride 是一种广谱的第三代氟喹诺酮类抗生素,是氧氟沙星的光学活性 L-异构体,具有抗菌活性。左氧氟沙星通过细菌细胞壁扩散并通过抑制 DNA 促旋酶(细菌拓扑异构酶 II)起作用,这是一种 DNA 复制、RNA 转录和细菌 DNA 修复所需的酶。 DNA 促旋酶活性的抑制导致细菌细胞生长受阻。
Type II topoisomerase inhibitor 1 可用于抗菌领域。Type II topoisomerase inhibitor 1 是大肠杆菌DNA 旋转酶的选择性抑制剂,IC50值为 1.7 nM,并能与 Asp73 残基形成氢键。Type II topoisomerase inhibitor 1 抑制拓扑异构酶 IV 的活性,IC50值为 0.98 μM。
TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topoIV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2].