By aiming to design new antimicrobial agents, we prepared new series of thiazolidin‐4‐ones(12a–d), imidazolin‐4‐ones(13a–d), and azetidin‐2‐ones (14a–d), having pyridine and pyrimidine moieties. Chemical structures of these derivatives were elucidated by the use of spectral and elemental analyses. All the new substituted pyridopyrimidines were subjected to in vitro antimicrobial testing by estimating the zone of inhibition toward Bacillus subtilis and Staphylococcus aureus, as examples of bacterial species, in addition to Aspergillus flavus and Candida albicans, as examples of fungal species. The results of antimicrobial testing detected that all the screened derivatives displayed antibacterial effect; especially azetidin‐2‐one derivative, (14c ), was the most active one. Regarding the antifungal potential, only thiazolidinone derivatives, 12a and 12c, and the imidazolinone, 13c, displayed inhibitory activity toward Aspergillus flavus , while all the tested compounds, 12a–d , 13a–d, and 14a–d, except 14a, produced inhibitory potential toward Candida albicans . Docking studies of the most active antimicrobial agents, 12c, 13c, and 14c, within GLN‐6‐P, recorded good scores with several binding interactions with the active site.

中文翻译：

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制备具有吡啶和嘧啶部分并具有抗菌活性的新型噻唑烷酮，咪唑啉酮和氮杂环丁酮

通过设计新的抗菌剂，我们制备了新的噻唑烷丁-4-酮（12a-d），咪唑啉-4-酮（13a-d）和氮杂环丁烷-2-酮（14a-d），它们具有吡啶和嘧啶部分。这些衍生物的化学结构通过光谱和元素分析得以阐明。除黄曲霉菌和白色念珠菌外，所有新的取代的吡啶并嘧啶类均通过体外对枯草芽孢杆菌和金黄色葡萄球菌（作为细菌种类的实例）的抑制区域进行了体外抗菌测试，作为真菌种类的例子。抗菌测试结果表明，所有筛选出的衍生物均具有抗菌作用。尤其是azetidin-2-one衍生物（14c）是最活跃的衍生物。关于抗真菌潜力，只有噻唑烷酮衍生物12a和12c以及咪唑啉酮13c表现出对黄曲霉的抑制活性，而所有测试化合物12a–d，13a–d和14a–d除14a均具有抑制作用。对白色念珠菌的潜力。最有效的抗菌剂的对接研究，GLN-6-P中的12c，13c和14c记录了良好的成绩，并且与活性位点发生了多次结合相互作用。