目的 設(shè)計(jì)并合成異 唑衍生物，并對(duì)其體外抗菌活性進(jìn)行了初步評(píng)價(jià)。方法 以3,4-二氟苯甲醛、鹽酸羥胺為起始原料，經(jīng)多步反應(yīng)合成目標(biāo)化合物。以利奈唑胺為陽(yáng)性對(duì)照藥，對(duì)目標(biāo)化合物的抗菌活性進(jìn)行評(píng)價(jià)。結(jié)果 合成了9個(gè)新化合物，其結(jié)構(gòu)經(jīng)1H-NMR、MS確證，體外活性測(cè)試結(jié)果顯示，有1個(gè)化合物有顯著的抗菌活性，與利奈唑胺相當(dāng)。結(jié)論 體外活性試驗(yàn)表明，含異 唑的所制備化合物作為新型的抗菌劑，其構(gòu)效關(guān)系值得進(jìn)一步研究。

Objective To design and synthesize antibacterial derivatives containing isoxazoline. and to evaluate their antibacterial activities. Methods The target compounds were synthesized with the starting material 3, 4-difluoro-benzaldehy with hydroxylamine hydrochloride. And their antibacterial activities have been tested in vitro with linezolide as positive control. Results Nine target compounds were synthesized and their structures were confirmed by 1H-NMR, MS. The pharmacological tests showed that one of the tested compounds exhibited novel antibacterial activity compared with linezolide. Conclusion The structure-activity relationships of isoxazoline derivatives, as a novel antibaterial type, should be further investigated.

天津市科委基礎(chǔ)科學(xué)重點(diǎn)資助項(xiàng)目（033801911）