A number of novel pyrazole derivatives have been synthesized, and several of these compounds are potent antibacterial agents with minimum inhibitory concentrations as low as 0.5 μg/mL. Human cell lines were tolerant to these lead compounds, and they showed negligible hemolytic effects at high concentrations. These bactericidal compounds are very effective against bacterial growth in both planktonic and biofilm contexts. Various techniques were applied to show the inhibition of biofilm growth and eradication of preformed biofilms by lead compounds. Potent compounds are more effective against persisters than positive controls. In vivo studies revealed that lead compounds are effective in rescuing C. elegans from bacterial infections. Several methods were applied to determine the mode of action including membrane permeability assay and SEM micrograph studies. Furthermore, CRISPRi studies led to the determination of these compounds as fatty acid biosynthesis (FAB) inhibitors.

中文翻译：

---

4-[4-(苯胺甲基)-3-苯基吡唑-1-基]苯甲酸衍生物脂肪酸生物合成抑制剂的开发及其抗菌性能

已经合成了许多新型吡唑衍生物，其中一些化合物是有效的抗菌剂，最低抑制浓度低至 0.5 μg/mL。人类细胞系对这些先导化合物具有耐受性，并且在高浓度下表现出可忽略不计的溶血作用。这些杀菌化合物对于浮游和生物膜环境中的细菌生长非常有效。应用各种技术来显示先导化合物对生物膜生长的抑制和对预先形成的生物膜的根除。有效的化合物比阳性对照更能有效地对抗持续者。体内研究表明，先导化合物可以有效地拯救秀丽隐杆线虫免受细菌感染。应用多种方法来确定作用方式，包括膜渗透性测定和 SEM 显微照片研究。此外，CRISPRi 研究确定了这些化合物作为脂肪酸生物合成 (FAB) 抑制剂。