五环三萜。第5部分：作为糖原磷酸化酶抑制剂的科罗索酸衍生物的合成与构效关系研究
Pentacyclic triterpenes. Part 5: synthesis and SAR study of corosolic acid derivatives as inhibitors of glycogen phosphorylases.
作者信息
Wen Xiaoan, Xia Jun, Cheng Keguang, Zhang Liying, Zhang Pu, Liu Jun, Zhang Luyong, Ni Peizhou, Sun Hongbin
机构信息
Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China.
出版信息
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5777-82. doi: 10.1016/j.bmcl.2007.08.057. Epub 2007 Aug 28.
The synthesis and biological evaluation of corosolic acid derivatives and related compounds as inhibitors of rabbit muscle glycogen phosphorylase a is described. Within this series of compounds, 8 (IC(50)=7.31 microM), 12d (IC(50)=3.26 microM), and 12e (IC(50)=5.1 microM) exhibited more potent activities than the parent compound 1 (IC(50)=20 microM). SAR of these compounds is also discussed.
本文描述了熊果酸衍生物及相关化合物作为兔肌肉糖原磷酸化酶a抑制剂的合成及生物学评价。在这一系列化合物中，8（IC(50)=7.31微摩尔）、12d（IC(50)=3.26微摩尔）和12e（IC(50)=5.1微摩尔）表现出比母体化合物1（IC(50)=20微摩尔）更强的活性。还讨论了这些化合物的构效关系。
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