摘要
目的设计并合成一系列2-萘基乙胺类化合物,研究其减肥作用。方法以7-甲氧基-1-萘满酮为原料,经多步反应合成目标化合物。培养前脂肪细胞3T3-L1,油红O染色法检测各目标化合物对3T3-L1分化的影响,并进一步研究化合物N-1-[1-(7-甲氧基-1-萘基)环丁基]-3-甲基丁基-N,N-二甲胺(9 c)对饮食诱导的肥胖大鼠的减肥作用。结果合成了9个未见文献报道的目标化合物,其结构均经过1H-NMR及MS谱确证。化合物(9 c)在浓度较高时有一定的减肥降脂作用。结论侧链碳上烃基体积增大,脂溶性增强,减肥作用增强;氮上为给电子基团时,碱性提高,减肥作用增强;氮上为吸电子基团时基本没有活性。
Objective To design and synthesize a series of 2-naphthyl ethylamine derivatives and to evaluate their anti-obesity effect.Methods The target compounds were synthesized in several steps starting from 7-methoxy-1-tetralone.3T3-L1 preadipocytes differentiation was observed by oil red O staining.1-[1-（7-methoxynaphthalen-1-yl）cyclo-butyl]-N,N,3-trimethylbutan-1-amine（9c） was selected for the evaluation of obesity controlling effect in rats susceptible to diet-induced obesity.Results Nine compounds were synthesized and they all were first reported.All the structures were confirmed by 1H-NMR and MS.Compound（9c） had some anti-obesity activity at high concentration.Conclusion The anti-obesity effect enhanced with the size increase of alkyl on the side chain.If the substituent groups of N-atom are electron-donating groups,the anti-obesity effect improves.When the substituent groups of N-atom are electron-withdrawing groups,the anti-obesity effect almost disappears.
出处
《中南药学》
CAS
2009年第12期900-904,共5页
Central South Pharmacy
关键词
肥胖
2-萘基乙胺
减肥作用
obesity 2-naphthyl ethylamine anti-obesity effect
