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目的设计合成O5′,N6-双取代腺苷衍生物,并评价其降血脂活性,寻找新型降血脂化合物。方法以6-氯嘌呤为起始原料,经4步反应合成目标化合物;通过测试目标化合物对油酸刺激下HepG2细胞内三酰甘油水平的影响及高胆固醇血脂症小鼠总胆固醇含量的影响评价化合物的活性。结果与结论合成了12个未见文献报道的新化合物,其结构经1H-NMR和MS谱确证。活性评价结果显示,多数化合物表现出良好的降血脂活性。
OBJECTIVE To design and synthesize O5 ’, N6-disubstituted adenosine derivatives and evaluate their hypolipidemic activity to find novel hypolipidemic compounds. Methods The target compounds were synthesized by 4-step reaction using 6-chloropurine as the starting material. The effect of the target compound on triacylglycerol level in HepG2 cells stimulated by oleic acid and the total cholesterol content in hypercholesterolemic mice Compound activity. RESULTS AND CONCLUSIONS Twelve new compounds were synthesized and their structures were confirmed by 1H-NMR and MS spectra. Activity evaluation showed that most compounds showed good hypolipidemic activity.