化学
咪唑
乙酰胺
抗菌活性
芳基
对接(动物)
盐酸盐
大肠杆菌
抗菌剂
核化学
烷基
组合化学
立体化学
有机化学
药物化学
细菌
生物化学
基因
遗传学
护理部
医学
生物
作者
Ahmed M. M. El‐Saghier,Aly Abdou,Mounir A. A. Mohamed,Hany M. Abd El‐Lateef,Asmaa M. Kadry
出处
期刊:ACS omega
[American Chemical Society]
日期:2023-08-09
卷期号:8 (33): 30519-30531
被引量:6
标识
DOI:10.1021/acsomega.3c03767
摘要
El-Saghier reaction is the novel, general, and green reaction of various amines with ethyl cyanoacetate and ethyl glycinate hydrochloride. A new series of imidazolidin-4-ones and bis-N-(alkyl/aryl) imidazolidin-4-ones was synthesized in a sequential, one-pot procedure under neat conditions for 2 h at 70 °C. Excellent high yields (90-98%) were achieved in a short period of time while avoiding issues related to the hazardous solvents utilized (cost, safety, and pollution). The spectrum analyses and elemental data of the newly synthesized compounds helped us to clarify their structures. The obtained compounds were tested for antibacterial activity in vitro and compared to the standard antibiotic chloramphenicol as the standard, measuring the inhibition zone (nm) and activity index (%). With an antibacterial percentage value of 80.0 against Escherichia coli, N,N'-(propane-1,3-diyl) bis(2-(4-oxo-4,5-dihydro-1H-imidazole-2-yl) acetamide) proved to be the most effective. Antimicrobial activity was confirmed by a molecular docking investigation to investigate how chemicals bind to the bacterial FabH-CoA complex in E. coli (PDB ID: 1HNJ).
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