1404481-52-2Relevant academic research and scientific papers
Synthesis and anti-biofilm activities of dihydro-pyrrol-2-one derivatives on Pseudomonas aeruginosa
Ye, Yong,Fang, Fei,Li, Yue
supporting information, p. 597 - 601 (2015/03/05)
Biofilm formation is an important reason for bacterial resistance to antimicrobials. Many compounds with dihydro-pyrrol-2-one (DPO) have antibacterial effects. It is prospective to base on DPO skeleton to design new compounds for biofilm inhibition. DPO was designed by a novel method of tandem cyclization between ethyl glyoxalate and amines, the series of DPO derivatives were synthesized by change of the amines. Their activities were evaluated by the inhibition of biofilm in Pseudomonas aeruginosa. The interaction of DPO derivatives with mannitol dehydrogenase (MDH) or extracellular DNA (eDNA) in the biofilm was simulated by molecular docking to reveal possible mechanism. 19 new DPO derivatives were synthesized and identified, 15 of them had antibacterial activities, but only 5 of them had more than 50% inhibition on biofilm of P. aeruginosa at 50 μg/mL. The MDH activity and eDNA content in biofilm decreased significantly after treatment of the DPO derivatives in concentration dependence. The simulation reveals that strong interaction exists between the five DPO derivatives and MDH or eDNA, which are involved in anti-biofilm mechanism. The synthetic method of DPO derivatives is practical to provide effective anti-biofilm agents for P. aeruginosa, and they take effect through inhibition on MDH and eDNA of biofilm.
Synthesis of functionalized 2-pyrrolidinones via domino reactions of arylamines, ethyl glyoxylate and acetylenedicarboxylates
Gao, Hong,Sun, Jing,Yan, Chao-Guo
supporting information, p. 589 - 594 (2013/07/27)
An efficient and practical synthetic method for the functionalized 2-pyrrolidinones was successfully developed via the domino reactions of ethyl glyoxylate and acetylenedicarboxylate with 2 M arylamines in the presence of benzoic acid as catalyst. When tw
Pd-catalyzed tandem cyclization of ethyl glyoxalate and amines: Rapid assembly of highly substituted cyclic dehydro-α-amino acid derivatives
Luo, Yueting,Lu, Xiaoxia,Ye, Yong,Guo, Ya,Jiang, Huanfeng,Zeng, Wei
supporting information, p. 5640 - 5643 (2013/01/15)
A novel cascade cyclization of ethyl glyoxalate and amines proceeds in the presence of Pd(TFA)2 (5 mol %) to give the cyclic dehydro-α-amino acid derivatives. This method provides a fast and simple access to highly substituted dihydro-pyrrol-2-ones in good yields.
