喹啉酮作为甲硫氨酰 - tRNA合成酶抑制剂的设计与合成
Design and synthesis of quinolinones as methionyl-tRNA synthetase inhibitors.
作者信息
Kim Su Yeon, Yoon Eun-Jeong, Choi Eung-Chil, Kim Sunghoon, Kang Taehee, Samrin Farhana, Puri Sadhna, Lee Jeewoo
机构信息
Laboratory of Medicinal Chemistry, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Shinlim-Dong, Seoul 151-742, Republic of Korea.
出版信息
Bioorg Med Chem. 2006 Nov 1;14(21):7154-9. doi: 10.1016/j.bmc.2006.06.062. Epub 2006 Jul 18.
Five new structural analogues of substituted-1H-quinolinones (19, 20, 23, 24, and 26) have been synthesized and evaluated for Staphylococcus aureus methionyl-tRNA synthetase enzyme inhibitory activity. These compounds were also tested against pathogens of six S. aureus, two Enterococcus faecalis, and one Enterococcus faecium. Among all the synthesized quinolinones, compound 20 displayed significant inhibitory activities in the strains of E. faecalis and E. faecium.
已合成了5种取代-1H-喹啉酮的新结构类似物（19、20、23、24和26），并对其进行了金黄色葡萄球菌甲硫氨酰-tRNA合成酶抑制活性评估。这些化合物还针对6株金黄色葡萄球菌、2株粪肠球菌和1株屎肠球菌的病原体进行了测试。在所有合成的喹啉酮中，化合物20在粪肠球菌和屎肠球菌菌株中表现出显著的抑制活性。
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