托品酮衍生物的合成及抗糖尿病活性

doi:10.3724/SP.J.1095.2013.20593

摘要/Abstract

摘要： 从6-羟基托品酮出发，经过羟基的乙酰基化和苯甲酰基化，再通过还原氨化高效地得到含有活泼胺基的2个母核化合物。 2个母核化合物与不同的酰氯反应，得到一系列托品酮衍生物。该衍生物经过体外过氧化物酶增生因子活化受体γ亚型（PPARγ）激活、二肽基肽酶Ⅳ （DPP-Ⅳ）抑制实验，发现多数化合物对DPP-Ⅳ显示抑制活性，其中2个化合物(3 μmol/L DMSO溶液)对DPP-Ⅳ抑制率超过30%。

关键词: 托品酮衍生物, 糖尿病, 体外, 二肽基肽酶IV抑制活性

Abstract: 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(PPARγ) 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 PPARγ of all compounds could be observed.

Key words: tropinone derivaties, diabetes, In-vitro model, dipeptidylpeptidase-IV inhibitory effect

中图分类号:

O629.3

谢朝阳, 李志伟, 鲍志超, 王建南, 尹鹏, 何侃, 颜霏, 郑群怡. 托品酮衍生物的合成及抗糖尿病活性[J]. 应用化学, DOI: 10.3724/SP.J.1095.2013.20593.

XIE Zhaoyang1, LI Zhiwei2, BAO Zhichao1, WANG Jiannan1, YIN Peng3, HE Kan1, YAN Fei1, ZHENG Qunyi1,4*. Synthesis and Antidiabetic Activity of Tropinone Derivatives[J]. Chinese Journal of Applied Chemistry, DOI: 10.3724/SP.J.1095.2013.20593.

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