A series of new N, N’-diarylurea derivatives were designed and synthesized, some of which exhibited potent antibacterial activity against the drug-susceptible and drug-resistant Gram-positive strains. Especially, compounds 2c, 2g-2l showed broader antibacterial spectrum and more potent antibacterial activity (MIC = 0.30–2.72 μM) against MRSA and MRSE than the control levofloxacin (MIC = 0.69–22.14 μM). In addition, compounds 2c, 2g, 2h and 2l exhibited much better antibacterial activity (MIC = 1.29–2.86 μM) against VRE (E. faecium) than sorafenib (MIC = 275.37 μM), PK150 (MIC = 5.07–10.13 μM) and SC78 (MIC = 2.40–4.79 μM). More importantly, the low cytotoxicity of compounds on cell lines HeLa and HepG2 implied a relatively wide therapeutic window, which was of high importance for further study.

设计并合成了一系列新的N,N'-二芳基脲衍生物，其中一些对药物敏感和耐药革兰氏阳性菌株表现出强效抗菌活性。尤其是化合物2c、2g - 2l对 MRSA 和 MRSE 表现出比对照左氧氟沙星 (MIC = 0.69–22.14 μM) 更广的抗菌谱和更强的抗菌活性 (MIC = 0.30–2.72 μM)。此外，化合物2c、2g、2h和2l对 VRE（粪肠球菌）的抗菌活性（MIC = 1.29–2.86 μM）比索拉非尼（MIC = 275.37 μM）、PK150 好得多(MIC = 5.07–10.13 μM) 和SC78 (MIC = 2.40–4.79 μM)。更重要的是，化合物对细胞系 HeLa 和 HepG2 的低细胞毒性意味着相对较宽的治疗窗口，这对于进一步研究具有重要意义。