3-(4-β-D-吡喃阿洛糖苷苯基)-4-胺羰基-5-甲氧羰基异噁唑衍生物的 合成及其镇静活性的研究

4-(β-D-吡喃阿洛糖苷)-α-氯代苯甲醛肟与N-芳基马来酰亚胺在三乙胺作用下, 以甲醇为溶剂, 通过1,3-偶极环加成, 合成了一系列未见文献报道的3-(4-β-D-吡喃阿洛糖苷苯基)-4-胺羰基-5-甲氧羰基异噁唑衍生物; 其结构经1H NMR, IR, MS (HRMS)加以确证. 并对4a～4h和5a进行了药理活性筛选, 结果表明, 部分化合物具有良好的镇静活性. 其中, 化合物4b (200 mg•kg－1), 4c (200 mg•kg－1), 4h (200 mg•kg－1), 与豆腐果苷相比较具有更强的活性.

Synthesis and Calm Activity of 3-(4-B-D-AIIopyranosyloxy-phenyl)-4-[(un)substituted anIlinocarbonyl]-5-methoxycarbonyl-isoxazoline Derivatives

A series of new 3-(4-β-D-allopyranosyloxyphenyl)-4-[(un)substituted anilinocarbonyl]-5-meth- oxycarbonyl-isoxazoline derivatives have been synthesized by the condensation between 4-β-D-allopyranosy- loxy-α-chloro-benzaldehydeoxime and N-[(un)substituted phenyl]maleimides with triethylamine in the metha-nol through a 1,3-dipolar cycloaddition reaction. The structures of all the new compounds were established by 1H NMR, IR, and MS (HRMS) techniques. The preliminary bioassay test of 4a～4h and 5a suggested that some of these compounds should show good calm activity. For example, compounds 4b (200 mg•kg－1), 4c (200 mg•kg－1) and 4h (200 mg•kg－1) were better than the parent helicid.