Synthesis and biological evaluation of novel pyrazolo[4,3-b]oleanane derivatives as inhibitors of glycogen phosphorylase |
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Authors: | Chen Jun Gong Yanchun Liu Jun Hua Weiyi Zhang Luyong Sun Hongbin |
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Affiliation: | Center for Drug Discovery, School of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, P. R. China. |
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Abstract: | Eighteen pyrazolo[4,3-b]oleanane derivatives have been synthesized and biologically evaluated as inhibitors of rabbit muscle GPa. Key compound 5 was readily obtained in four steps starting from oleanolic acid (OA; 1). Further modification based on pyrazolo triterpene 5 resulted in 17 novel pyrazolo pentacyclic triterpenes. All of the synthesized pyrazolo[4,3-b]oleanane derivatives were biologically assayed against rabbit muscle GPa. Within this series of compounds, pyrazole triterpene 19 (IC(50)=9.9 microM) exhibited more potent activity than the parent compound 1. Preliminary structure-activity relationship analysis of the pyrazolo[4,3-b]oleanane derivatives as GPa inhibitors is discussed. |
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Keywords: | Pyrazolo[4,3‐b]oleanane derivatives Glycogen phosphorylase (GPa) Triterpenes |
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