Jin Bo, Wang Tong, Chen Jia-Yi, Liu Xiao-Qing, Zhang Yi-Xin, Zhang Xiu-Ying, Sheng Zun-Lai, Yang Hong-Liang
Department of Veterinary Medicine, Northeast Agricultural University, Harbin, China.
Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, China.
Front Chem. 2022 Jul 18;10:949813. doi: 10.3389/fchem.2022.949813. eCollection 2022.
In this research, a series of 3-(pyridine-3-yl)-2-oxazolidinone derivatives was designed, synthesized, and evaluated for antibacterial activity, which included bacteriostatic, morphological, kinetic studies, and molecular docking. The results demonstrated that compounds , , and exhibited strong antibacterial activity similar to that of linezolid toward five Gram-positive bacteria. After observing the effect of the drug on the morphology and growth dynamics of the bacteria, the possible modes of action were predicted by molecular docking. Furthermore, the antibiofilm activity and the potential drug resistance assay was proceeded. These compounds exhibited universal antibiofilm activity and compound showed significant concentration-dependent inhibition of biofilm formation. Compound also showed a stable effect on (ATCC 49619) with less drug resistance growth for 15 days, which is much longer than that of linezolid. Overall, these results can be used to guide further exploration of novel antimicrobial agents.
在本研究中，设计、合成了一系列3-(吡啶-3-基)-2-恶唑烷酮衍生物，并对其抗菌活性进行了评估，包括抑菌、形态学、动力学研究以及分子对接。结果表明，化合物 、 、 和 对五种革兰氏阳性菌表现出与利奈唑胺相似的强抗菌活性。在观察药物对细菌形态和生长动力学影响后，通过分子对接预测了可能的作用模式。此外，还进行了抗生物膜活性和潜在耐药性测定。这些化合物表现出普遍的抗生物膜活性，化合物 对生物膜形成具有显著的浓度依赖性抑制作用。化合物 对 （ATCC 49619）也显示出稳定的效果，耐药性生长在15天内较少，这比利奈唑胺长得多。总体而言，这些结果可用于指导新型抗菌剂的进一步探索。
