衍生合成七种氮杂糖成分及其抑制α-葡萄糖苷酶构效关系分析

Synthesize seven azasugar derivatizatives and their structure-activity relationship on the inhibition of α-glucosidase

以白树(Suregada glomerulata)中分离得到的五个氮杂糖成分为底物,在其N上衍生合成,分析N上衍生基团对α-葡萄糖苷酶抑制活性的影响。分别合成了N-甲基化、N,N-二甲基化、N-丁基化和N-氧化衍生物,体外测试化合物的α-葡萄糖苷酶抑制活性。合成了7个未见文献报道的目标化合物,结构经1HNMR、13CNMR和MS确证。初步药理结果显示,所有衍生物均未见增强α-葡萄糖苷酶抑制活性。N-取代基对活性的影响较大;化合物5属于N,N-二取代衍生物,仍具有一定的α-葡萄糖苷酶抑制活性,值得进一步研究。

To synthesize the N-derivation of azasugars isolated from Suregada glomerulata .To analyze the N-substituent group affect the inhibit activity of α-glucosidase.N-methyl,N,N-dimethyl,N-butyl and N-oxidate derivatives were synthesized,and the bioactivity was tested in vitro aganist α-glucosidase.Seven compounds were synthesized,and the structure was confirmed by 1H NMR, 13 C NMR and MS.The preliminary pharmacological test results showed that all derivatives did not enhance the inhibitory activity.Compound 5 ,a N,N-derivative,possessed inhibitory activity against α-glucosidase,which is worthy for further study.