NATURAL PRODUCT RESEARCH AND DEVELOPMENT ›› 2019, Vol. 31 ›› Issue (7): 1216-1219. doi: 10.16333/j.1001-6880.2019.7.014

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

YAN Ren-yi1,LI Qiong-ya2,XU Bing2*,CHEN Ruo-yun1   

  1. 1Institute of Materia Medica,Chinese Academy of Medical Sciences & Peking Union Medical College,Beijing 100050,China; 2R & D,China Resources Sanjiu Medical & Pharmaceutical Co.,Ltd.,Shenzhen 518110,China
  • Online:2019-07-29 Published:2019-07-29

Abstract: 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,13C 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.

Key words: azasugar, Suregada glomerulata, &alpha, -glucosidase, inhibitory activity

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