引用本文:
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,
2013, 30(10): 1127-1132.
doi:
10.3724/SP.J.1095.2013.20593
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
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
托品酮衍生物的合成及抗糖尿病活性
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(3μmol/L DMSO溶液)对DPP-Ⅳ抑制率超过30%。
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关键词:
- 托品酮衍生物
- / 糖尿病
- / 体外
- / 二肽基肽酶Ⅳ抑制活性
English
Synthesis and Antidiabetic Activity of Tropinone Derivatives
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.
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