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由磺胺甲唑、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1HNMR、13CNMR、MS进行了表征。生物活性试验显示,低浓度范围,所得化合物不仅对蛋白质酪氨酸磷酸酶1B(PTP1B)和α-葡萄糖苷酶有一定抑制活性,而且对过氧化物酶体增殖物激活受体反应元件(PPRE)具有中等强度的激动活性,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%。
Thirteen unreported β-aminoketones were synthesized directly from the reaction of sulfamethoxazole, p-hydroxyacetophenone and aromatic aldehydes. The reaction selectivity occurred at α position of the carbonyl group. The product structure was characterized by 1HNMR, 13CNMR, MS. Bioactivity tests showed that, at low concentration range, the compounds obtained not only had a certain inhibitory activity on protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase, but also inhibit peroxisome proliferator-activated receptor response element (PPRE ) Had moderate intensity of agonistic activity, and the activity of 8 compounds was more than 40%, of which the activity of compound 11 reached 72.7%.