从6-羟基托品酮出发,经过羟基的乙酰基化和苯甲酰基化,再通过还原氨化高效地得到含有活泼胺基的2个母核化合物.2个母核化合物与不同的酰氯反应,得到一系列托品酮衍生物.该衍生物经过体外过氧化物酶增生因子活化受体γ亚型(PPARγ)激活、二肽基肽酶Ⅳ(DPP-Ⅳ)抑制实验,发现多数化合物对DPP-Ⅳ显示抑制活性,其中2个化合物(3 μmol/L DMSO溶液)对DPP-Ⅳ抑制率超过30％.
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