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Bis(azolyl)pyridine-2,6-dicarboxamide Derivatives: Synthesis, Bioassay Analysis and Molecular Docking Studies

机译:双(唑基)吡啶-2,6-二甲酰胺衍生物:合成、生物测定分析和分子对接研究

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摘要

A new class of bis(azolyl) pyridine-2,6-dicarboxamides based derivatives were designed and synthesized by employing ultrasonication methodology. In this work, we studied the role of different heteroaromatic azole units such as oxazole, thiazole and imidazole moieties along with different donating/withdrawing substituents on the pyridine scaffold and anticipated to display good biological activities. The detailed molecular docking studies validates the antimicrobial activities of these targeted molecules. Further, to evaluate their antioxidant properties, the target compounds were exposed to three different invitro free radical scavenging assay methods. Further, using the disc diffusion method, the targeted molecules were screened for invitro antibacterial activities against the pathogenic stains. Besides, the targeted molecules were also tested against A. niger and P. chrysogenum strains to assess their antifungal activity. The screening results reveals that, the most of the compounds form the series demonstrating reasonable to decent antioxidant and antimicrobial activities against pathogenic stains in comparison with the standard drug.
机译:采用超声方法设计合成了一类新型双(唑基)吡啶-2,6-二甲酰胺衍生物。本研究研究了不同杂芳香唑单元(如噁唑、噻唑和咪唑基团)以及不同供/撤取代基在吡啶支架上的作用,并有望表现出良好的生物活性。详细的分子对接研究验证了这些靶向分子的抗菌活性。此外,为了评估其抗氧化特性,将目标化合物暴露于三种不同的体外自由基清除测定方法。此外,采用圆盘扩散法筛选目标分子对致病性染色剂的体外抗菌活性。此外,还对靶分子进行了针对黑曲霉和产黄杨菌株的测试,以评估其抗真菌活性。筛选结果表明,与标准药物相比,该系列中的大多数化合物对致病性污渍表现出合理到不错的抗氧化和抗菌活性。

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