| γ-丁内酯类衍生物的合成及其脂肪酸合成酶抑制活性的研究 |
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| 引用本文： | 康建磊,郑志兵,王莉莉,王晓奎,李松.γ-丁内酯类衍生物的合成及其脂肪酸合成酶抑制活性的研究[J].中国药物化学杂志,2010,20(2):81-83,95. |
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| 作者姓名： | 康建磊 郑志兵 王莉莉 王晓奎 李松 |
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| 作者单位： | (1.国家食品药品监督管理局 药品审评中心，北京 100038；2.军事医学科学院 毒物药物研究所，北京 100850) ; |
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| 基金项目： | 国家自然科学基金项目(30672534) |
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| 摘 要： | 目的 以C75为先导化合物，设计、合成γ-丁内酯类衍生物，并研究其脂肪酸合成酶（fatty acid synthase, FAS）的抑制活性，以期发现新颖的FAS抑制剂。方法 以衣康酸酐为起始原料，经酯化、烃代、缩合/环合、水解4步反应合成目标化合物，采用体外方法初步筛选其FAS的抑制作用。结果与结论 合成了11个目标化合物，其结构经核磁和质谱确证；初步活性评价结果显示，含饱和烷烃侧链的化合物具有较好的FAS抑制活性，随侧链烷基的延长，其抑酶活性有增强的趋势。
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| 关 键 词： | γ-丁内酯类衍生物 化学合成 FAS抑制剂 |
| 收稿时间： | 2009-8-19 |
| 修稿时间： | 2009-1-20 |
Synthesis of γ-butyrolactone derivatives as FAS inhibitors |
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| KANG Jian-lei,ZHENG Zhi-bing,WANG Li-li,WANG Xiao-kui,LI Song.Synthesis of γ-butyrolactone derivatives as FAS inhibitors[J].Chinese Journal of Medicinal Chemistry,2010,20(2):81-83,95. |
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| Authors: | KANG Jian-lei ZHENG Zhi-bing WANG Li-li WANG Xiao-kui LI Song |
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| Institution: | (1. Center for Drug Evaluation, SFDA, Beijing 100038, China; 2. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China) |
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| Abstract: | Aim To design and synthesize a series of novel γ-butyrolactone derivatives with FAS（fatty acid synthase,FAS） inhibition activities,C75 as the lead compound.Methods The target compounds were synthesized from itaconic anhydride through a four-step process.The FAS inhibition activities were tested in vitro.Results and conclusion Eleven new compounds were synthesized,and their structures were confirmed by FAB-MS and 1H-NMR.The preliminary pharmacological testing results showed that ME-11、ME-12 and ME-13 have almost equal FAS inhibition activities to that of C75. |
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| Keywords: | γ-butyrolactone derivative chemical synthesis FAS inhibitor |
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