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Synthesis and Evaluation of Some Novel Chromone Based Dithiazoles as Antimicrobial Agents

机译:几种新型基于苯甲酮的二噻唑类抗菌剂的合成与评价

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摘要

Novel substituted 1,2,4-dithiazolylchromones >3a–j were synthesized by the reaction of 3-formylchromones (>1a–j) with two equivalents of p-chlorothiobenzamide (>2) in dry xylene and characterized spectroscopically (IR, 1H and 13C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains and were found to possess good to moderate inhibitory potential against all tested strains. Antimicrobial results reveal that compounds bearing lipophilic electron withdrawing groups such as chloro and bromo displayed significant inhibitory potential against both bacterial and fungal strains. Particularly, compound >3c displayed significant inhibitory against bacterial strains and compound >3h exhibits significant inhibitory potential in comparison to standard drug fluconazole against fungal strain S. cerevisiae.
机译:通过3-甲酰基色酮(> 1a–j )与两当量的对氯硫代苯甲酰胺(>)的反应合成了新型取代的1,2,4-二噻唑基色酮> 3a–j > 2 )在干燥的二甲苯中进行光谱表征(IR, 1 H和 13 C NMR,质量)和元素分析。筛选所有合成的化合物对各种致病细菌和真菌菌株的体外抗菌活性,发现它们对所有测试菌株均具有良好至中等的抑制潜力。抗菌结果表明,带有亲脂性吸电子基团(例如氯和溴)的化合物对细菌和真菌菌株均显示出显着的抑制潜力。特别地,与标准药物氟康唑相比,化合物> 3c 显示出对细菌菌株的显着抑制作用,化合物> 3h 显示出对真菌菌株S.cerevisiae的显着抑制潜力。

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