4-(3-(4-羟基苯基) -3-氧代-1-芳基丙氨基)-N-(5-甲基异噁唑-3-基)苯磺酰胺的合成与抗糖尿病活性

由磺胺甲噁唑、对羟基苯乙酮和芳香醛反应直接合成了13个未见报道的β-氨基酮，反应选择性发生在羰基α位。产物结构通过¹H NMR、¹³C NMR、MS进行了表征。生物活性试验显示，低浓度范围，所得化合物不仅显示一定的蛋白质酪氨酸磷酸酶1B(PTP1B)和α-葡萄糖苷酶抑制活性，而且具有中等强度的过氧化物酶体增殖物激活受体反应元件(PPRE)的激动活性，8个化合物的激动活性超过40％，其中化合物11的活性达到72.7％。

Synthesis and Preliminary Evaluation of Antidiabetic Activity of 4-(3-(4-Hydroxyphenyl)-3-oxo-1-arylpropylamino)-N-(5-Methylisoxazol-3-yl) Benzenesulfonamide

Thirteen new β-amino ketones were designed and synthesized directly through the Mannich reaction of sulfamethoxazole, 4-hydroxyacetophenone and aromatic aldehydes in good yields. The reaction selectively occurred at the α-position of the carbonyl group of 4-hydroxyacetophenone. Their chemical structures were confirmed by means of ¹H NMR, ¹³C NMR and MS. Biological activity tests showed that in the rage of low concentrations, these title compounds displayed a certain inhibitory activity against protein tyrosine phosphatase 1B(PTP1B) and α-glucosidase. Moreover, some could activate the peroxisome proliferator activated receptor response element(PPRE) moderately. The PPRE agonist activity of eight compounds was over 40%, among them compound 11 showed the highest activity(72.7%), which deserved further study.