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Development and Antibacterial Properties of 4-[4-(Anilinomethyl)-3-phenylpyrazol-1-yl]benzoic Acid Derivatives as Fatty Acid Biosynthesis Inhibitors
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2023-09-20 , DOI: 10.1021/acs.jmedchem.3c00969 Subrata Roy 1 , Hansa Raj Kc 1 , Justin Roberts 1 , Jared Hastings 1 , David F Gilmore 2 , Robert C Shields 2 , Mohammad A Alam 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2023-09-20 , DOI: 10.1021/acs.jmedchem.3c00969 Subrata Roy 1 , Hansa Raj Kc 1 , Justin Roberts 1 , Jared Hastings 1 , David F Gilmore 2 , Robert C Shields 2 , Mohammad A Alam 1
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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-（苯胺基甲基）-3-苯基吡唑-1-基]苯甲酸衍生物作为脂肪酸生物合成抑制剂的开发及抑菌性能
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，并且在高浓度下显示出可忽略不计的溶血作用。这些杀菌化合物在浮游生物和生物膜环境中对细菌生长都非常有效。应用了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。强效化合物比阳性对照对持久性更有效。体内研究表明，铅化合物可有效拯救秀丽隐杆线虫免受细菌感染。应用了几种方法来确定作用方式，包括膜通透性测定和 SEM 显微照片研究。此外，CRISPRi 研究导致这些化合物被确定为脂肪酸生物合成 （FAB） 抑制剂。
更新日期：2023-09-20
中文翻译：
4-[4-（苯胺基甲基）-3-苯基吡唑-1-基]苯甲酸衍生物作为脂肪酸生物合成抑制剂的开发及抑菌性能
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，并且在高浓度下显示出可忽略不计的溶血作用。这些杀菌化合物在浮游生物和生物膜环境中对细菌生长都非常有效。应用了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。强效化合物比阳性对照对持久性更有效。体内研究表明，铅化合物可有效拯救秀丽隐杆线虫免受细菌感染。应用了几种方法来确定作用方式，包括膜通透性测定和 SEM 显微照片研究。此外，CRISPRi 研究导致这些化合物被确定为脂肪酸生物合成 （FAB） 抑制剂。
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