中氮茚并喹啉二酮衍生物的合成、表征及抗菌活性

Synthesis,Characterization and Antimicrobial Activity of Indolizinoquinoline-5,12-dione Derivatives

以自制的6,7-二氯喹啉-5,8-二酮为原料,经一步反应合成了目标化合物9-氯-5,12-二酮-5,12-二氢中氮茚并[2,3-g]喹啉-6-甲酸乙酯,并通过~1HNMR、HRMS以及X-射线单晶衍射对其结构进行表征。活性测试结果表明,该化合物对革兰氏阳性菌具有选择性抑制作用,对耐甲氧西林金黄色葡萄球菌(MRSA)的最小抑菌浓度(MIC)为1μg/mL,优于阳性对照药物万古霉素。通过化合物与DNA促旋酶的分子对接实验进一步说明了化合物可能的作用机理。

Target compound of ethyl 9-chloro-5,12-dioxo-5,12-dihydroindolizino[2,3-g]quinoline-6-carboxylate was one-step synthesized from the homemade 6,7-dichloroquinoline-5,8-dione.The atomic structure was characterized using 1HNMR,HRMS,and X-ray single crystal analysis.Antimicrobial activity assessment indicates that the compound exhibits selective inhibition against gram-positive bacterial strains.Meanwhile,its minimum inhibition concentration（MIC） against methicillin-resistant Staphylococcus aureus（MRSA） is 1 μg/mL,which is superior to that of positive control：vancomycin.Furthermore,we proposed the inhibition mechanism via docking the compound to DNA gyrase.