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设计合成了具有降血糖活性的3-甲基-1-苯基-4-[4-[[5-甲基-2-(4-取代芳基)-噁唑-4-基]甲氧基]-芳亚甲(苄)基]}-2-吡唑啉-5-酮类化合物.用丁二酮单肟和(取代的)苯甲醛环合、氯化得到氯甲基噁唑衍生物,与对羟基苯甲醛或香兰醛缩合,再与3-甲基-1-苯基-2-吡唑啉-5-酮进行Knoevenagel反应及催化氢化得到目标化合物(Ⅰ和Ⅱ),共合成了16个未见文献报道的新化合物,并利用元素分析、IR、MS和1HNMR确证了化合物的结构.初步药理试验结果表明,所合成的化合物有抑制血糖升高的倾向以及能明显加强和延长外源性胰岛素的降血糖作用,其中化合物Ⅰb,Ⅰd和Ⅰf尤为突出,说明这类化合物可能有增强胰岛素敏感性的作用.
Design and synthesis of 3-methyl-1-phenyl-4- [4- [[5-methyl-2- (4-substituted aryl) -oxazol-4-yl] methoxy ] - arylmethylene (benzyl)]} - 2-pyrazolin-5-one Compounds were cyclized with diacetylmonooxime and (substituted) benzaldehyde to give the chloromethyloxazole derivative , Condensation with p-hydroxybenzaldehyde or vanillin, and Knoevenagel reaction and catalytic hydrogenation with 3-methyl-1-phenyl-2-pyrazolin-5-one to obtain the target compounds (I and II) Sixteen novel compounds were reported, and their structures were elucidated by elemental analysis, IR, MS and 1HNMR.The results of preliminary pharmacological experiments showed that the synthesized compounds have the tendency of inhibiting the increase of blood glucose, as well as significantly strengthening and prolonging The hypoglycemic effects of exogenous insulin, compounds Ib, Id and If are particularly prominent, indicating that these compounds may have increased insulin sensitivity.