根据生物电子等排原理，以2，3，4-三氟苯甲酸为原料，经硝化、还原、氧化和亲核取代反应制得中间体2-（2，3，4-三氟-5-硝基苯）-1，3-二氧戊环（4）；4分别经7步反应合成了12个新型的苯并噁唑酮或苯并咪唑酮螺嘧啶三酮类化合物（12a～12f，19a～19f），其结构经1H NMR，13C NMR和ESI-MS表征。采用CLSI标准研究了12和19对甲氧西林耐药金黄色葡萄球菌（ A）、甲氧西林耐药表皮葡萄球菌（ B）、青霉素耐药肺炎链球菌（ C）和化脓性链球菌（D）的体外抗菌活性。结果表明：12的抗菌活性优于19，其中12a的抗菌活性最好，对A～D的MIC值分别为8～16μg· mL－1。%According to the principle of bioisosteric, an intermediate[2-(2,3,4-trifluoro-5-nitroben-zene)-1,3-dioxolame(4)] was prepared by the reaction of nitration, reduction, oxidation and nucleo-philic substitution from 2,3,4-trifluorobenzoic acid.Twelve novel spiropyrimidinetrione compounds containing benzoxazolinone or benzimidazolone(12a~12f, 19a~19f) were synthesized by a seven-step reaction from 4.The structures were characterized by 1 H NMR, 13 C NMR and ESI-MS.The anti-bacterial activities of 12 and 19 against methicillin-resistant Ataphylococcus aureus( A) , methicillin-re-sistant Staphylococcus epidermidis( B) , penicillin-resistant Streptococcus pneumonia( C) and Streptococ-cus pyogenes( D) were investigated by CLSI standard.The results indicated that the antibacterial activi-ties of 12 were better than 19.12a exhibited best activities with MIC of 8~16 μg· mL-1 .
展开▼
