化学
体内
细菌
苯甲酸
铅化合物
生物合成
生物膜
细菌细胞结构
脂肪酸
吡唑
最小抑制浓度
生物化学
细菌生长
抗菌活性
抗菌剂
体外
立体化学
抗生素
酶
生物
遗传学
生物技术
作者
Subrata Roy,Hansa Raj Kc,Justin Roberts,J. Woodland Hastings,David F. Gilmore,Robert C. Shields,Mohammad A. Alam
标识
DOI:10.1021/acs.jmedchem.3c00969
摘要
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.
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