苯酞类化合物的制备及其抑制胰脂肪酶活性研究

Synthesis and Inhibiting Activities on Pancreatic Lipase of Novel Phthalide Compounds

奥利司他是到目前为止市场上唯一的脂肪酶抑制剂类减肥药。本文参考奥利司他与胰脂肪酶的单晶复合物,通过计算机辅助药物设计Docking方法,设计并合成了9个具有长疏水侧链的苯酞类新化合物。化合物结构通过HRESIMS、1 H NMR、13 C NMR确证。对其抑制胃肠道胰脂肪酶的活性进行了初步测定,1mg/mL的化合物2,5,7对胰脂肪酶活性抑制率分别达到了49%,30%,35%。

Orlistat is by far the only anti-obesity drug of pancreatic lipase on the market.Nine novel phthalide compounds with long lipid chains were designed and synthesized.All new compounds were characterized by 1H-NMR,（13）C-NMR,high resolution electrospray ionization mass.Inhibiting activities on pancreatic lipase of synthesized compounds were tested,and compound 2,5,7show 49%,30% and 35%inhibition rate on pancreatic lipase at the concentration of 1mg/mL.