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Synthesis and Evaluation of 5-imino-4-thioxoimidazolidin-2-one Derivatives as Antibacterial and Antifungal Agents
Medicinal Chemistry ( IF 1.9 ) Pub Date : 2021-06-30 , DOI: 10.2174/1573406416666191227112648
Samir Y Abbas 1 , Marwa A M Sh El-Sharief 2 , Reem A K Al-Harbi 3 , Eman W El-Gammal 4 , Ahmed M S El-Sharief 5
Affiliation  

Objective: It was interesting to synthesize some new 5-imino-4-thioxoimidazolidin-2- one derivatives with different halogenated and alkylated aromatic substituents at N-(1) and N-(3) and evaluation of their expected antibacterial and antifungal activities.

Methods: New 5-imino-4-thioxoimidazolidin-2-one derivatives were synthesized through the reaction of different halogenated and alkylated N-arylcyanothioformamides with halogenated and alkylated aryl isocyanates.

Results: 5-Imino-4-thioxoimidazolidin-2-ones were obtained in high yields with excellent purity. The activities of imidazolidines as antibacterial and antifungal agents were studied. Some of the imidazolidine derivatives displayed significant antibacterial and antifungal activities.

Conclusion: 5-Imino-4-thioxoimidazolidin-2-ones were obtained in 77-90% yields with excellent purity. The antibacterial and antifungal activities suggest that some of the imidazole derivatives possess significant antimicrobial activity against B. subtilis, K. pneumonia and C. albicans and moderate activity against S. aureus.



中文翻译:

作为抗菌和抗真菌剂的 5-imino-4-thioxoimidazolidin-2-one 衍生物的合成与评价

目的:合成一些在 N-(1) 和 N-(3) 处具有不同卤化和烷基化芳族取代基的新型 5-imino-4-thioxoimidazolidin-2-one 衍生物并评估其预期的抗菌和抗真菌活性是很有趣的。

方法:通过不同卤化和烷基化的N-芳基氰基硫代甲酰胺与卤化和烷基化的异氰酸芳基酯反应,合成了新的5-imino-4-thioxoimidazolidin-2-one衍生物。

结果: 5-Imino-4-thioxoimidazolidin-2-ones 以高收率和优异的纯度获得。研究了咪唑烷作为抗菌剂和抗真菌剂的活性。一些咪唑烷衍生物显示出显着的抗菌和抗真菌活性。

结论: 5-Imino-4-thioxoimidazolidin-2-ones 以 77-90% 的产率获得,纯度极佳。抗菌和抗真菌活性表明,某些咪唑衍生物对枯草芽孢杆菌、肺炎克雷伯菌和白色念珠菌具有显着的抗菌活性,对金黄色葡萄球菌具有中等活性。

更新日期:2021-06-08
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