新型异噁唑衍生物的合成及其抗菌活性

Synthesis and Antibacterial Activities of New Isoxazoline Derivatives

5-乙酰胺甲基-3-[3-氟-4-(1-哌嗪基苯基)]异噁唑啉与氯乙酰氯反应制得中间体5-乙酰胺甲基-3-[3-氟-4-(4-氯乙酰基-1-哌嗪基苯基)]异噁唑啉(2);2与取代哌嗪或取代六氢吡啶反应合成了15个新型的异噁唑类衍生物(4a～4o),其结构经1H NMR和FAB-MS表征。初步的生物活性测试结果表明,4a～4o对金黄色葡萄球菌、藤黄八叠球菌、绿脓假单胞菌和肺炎克雷伯杆菌均有一定的抗菌活性。

Intermediate,5-（acetamidomethyl）-3-[3-fluoro-4-（4-chloroacetyl-4- piperazinyl）phenyl]isoxaline（2）,was obtained by the reaction 5- acetamidomethyl-3-[3-fluoro-4-（1-piperazynyl）]isoxaline with chloroacetyl chloride.Fifteen new isoxazoline derivatives（4a-4o） were synthesized by the reaction of 2 with substituted-piperazine or substituted-hexhydropyridine.The preciminary antibacterial activity tests showed that 4a-4o exhibited good antibacterial activities against S.aureus 26003,Sarcina lutea 28001,P.aeruginosa 10211 and K.pneumoniae 46117.