Synthesis and Biological Evaluation of Novel Pyrazolo[4,3‐ b ]oleanane Derivatives as Inhibitors of Glycogen Phosphorylase | Zendy

Chen Jun | Zendy; Gong Yanchun | Zendy; Liu Jun | Zendy; Hua Weiyi | Zendy; Zhang Luyong | Zendy; Sun Hongbin | Zendy

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Synthesis and Biological Evaluation of Novel Pyrazolo[4,3‐ b ]oleanane Derivatives as Inhibitors of Glycogen Phosphorylase

Author(s) -

Chen Jun,

Gong Yanchun,

Liu Jun,

Hua Weiyi,

Zhang Luyong,

Sun Hongbin

Publication year - 2008

Publication title -

chemistry and biodiversity

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.427

H-Index - 70

eISSN - 1612-1880

pISSN - 1612-1872

DOI - 10.1002/cbdv.200890117

Subject(s) - oleanane , chemistry , oleanolic acid , triterpene , biological activity , stereochemistry , terpene , glycogen phosphorylase , biochemistry , enzyme , in vitro , medicine , alternative medicine , pathology

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 μ M ) 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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