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Assessment of novel pyrazolopyridinone fused imidazopyridines as potential antimicrobial agents

机译:新型吡唑并吡啶酮与咪唑并吡啶类化合物作为潜在抗菌剂的评估

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摘要

The antimicrobial activity of pyrazolopyridinone fused imidazopyridines was investigated against various Gram-positive and Gram-negative bacteria as well as fungal strains using Ofloxacin and Fluconazole as positive controls, respectively. Interestingly, all the derivatives displayed good to excellent antibacterial activities against all bacterial strains with MIC values ranging from 25 to 0.39?μg/mL; compounds 3aA and 4dA displaying even better activity against Staphylococcus epidermidis than the positive control (MIC?=?1.25?μg/mL). These derivatives also proved to be effective antifungal agents with MICs ranging from 12.5 to 0.39?μg/mL; compounds, 3aA and 4dA being most potent antifungal representatives against Candida albicans in comparison to the reference drug Fluconazole (MIC?=?0.39?μg/mL). The SARs associated with different diversity points of these derivatives have also been discussed. Graphical abstract Display Omitted.
机译:分别使用氧氟沙星和氟康唑作为阳性对照,研究了吡唑并吡啶并酮融合的咪唑并吡啶对各种革兰氏阳性和革兰氏阴性细菌以及真菌菌株的抗菌活性。有趣的是,所有衍生物对所有细菌菌株均表现出良好至优异的抗菌活性,MIC值在25至0.39?g / mL之间。化合物3aA和4dA对表皮葡萄球菌显示出比阳性对照更好的活性(MIC≥1.25≤μg/ mL)。这些衍生物也被证明是有效的抗真菌剂,MIC范围为12.5至0.39?g / mL。与参考药物氟康唑相比,化合物3aA和4dA是最有效的抗白色念珠菌的抗真菌代表(MIC?=?0.39?μg/ mL)。还讨论了与这些导数的不同分集点相关的SAR。图形抽象显示被忽略。

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