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Citation: XIE Zhaoyang, LI Zhiwei, BAO Zhichao, WANG Jiannan, YIN Peng, HE Kan, YAN Fei, ZHENG Qunyi. Synthesis and Antidiabetic Activity of Tropinone Derivatives[J]. Chinese Journal of Applied Chemistry, ;2013, 30(10): 1127-1132. doi: 10.3724/SP.J.1095.2013.20593 shu

Synthesis and Antidiabetic Activity of Tropinone Derivatives

XIE Zhaoyang ^a, ,
LI Zhiwei ^b ,
BAO Zhichao ^a ,
WANG Jiannan ^a ,
YIN Peng ^c ,
HE Kan ^a ,
YAN Fei ^a ,
ZHENG Qunyi ^a,d

a. Herbalife Natsource(Hunan) Natual Products Corporation, Changsha 410100, China;
b. School of Chemistry and Biological Engineering, Changsha University of Science & Technology, Changsha 410114, China;
c. Natsource Chemical(Changsha) Corporation, Changsha 410329, China;
d. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China

Received Date: 18 December 2012
Revised Date: 15 February 2013

6-Hydroxytropinone was chosen as the primary precursor and subjected to a series of reactions including acetylation or benzoylation of its hydroxyl group,reduction and ammoniation of its keto group to yield two compounds containing tropane with primary amine core structure. A series of N-acyl compounds has been prepared by the reactions of the core structures with a variety of acyl chlorides. These compounds were screened in peroxisome proliferateive activeated recaptor-γ(PPAR_γ) and dipeptidylpeptidase-Ⅳ(DPP-Ⅳ) in-vitro models. Most of these compounds displayed inhibitory effect against DPP-Ⅳ and two of them showed inhibitory rates higher than 30% at 3 μmol/L in DMSO. But no activation toward PPAR_γ of all compounds could be observed.
- tropinone derivaties,
- diabetes,
- in-vitro model,
- dipeptidylpeptidase-Ⅳ inhibitory effect
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