Synthesis and glycosidase inhibition of C-7 modified casuarine derivatives  

Synthesis and glycosidase inhibition of C-7 modified casuarine derivatives

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作  者:Bin Cheng Yuki Hirokami Yi-Xian Li Atsushi Kato Yue-Mei Jia Chu-Yi Yu 

机构地区:[1]Beijing National Laboratory for Molecular Science(BNLMS),CAS Key Laboratory of Molecular Recognition and Function,CAS Research/Education Center forExcellence in Molecular Sciences,Institute of Chemistry,Chinese Academy of Sciences,Beijing 100190,China [2]University of Chinese Academy of Sciences,Beijing 100049 China [3]Department of Hospital Pharmacy,University of Toyama,Toyama 930-0194,Japan [4]National Engineering Research Center for Carbohydrate Synthesis,Jiangxi Normal University,Nanchang 320022,China

出  处:《Chinese Chemical Letters》2017年第8期1701-1704,共4页中国化学快报(英文版)

基  金:Financial support from the National Natural Science Foundation of China(Nos.21642012 and 21272240);National Science and Technology Major Projects for“Major New Drugs Innovation and Development”(No.2013ZX09508104);National Engineering Research Center for Carbohydrate Synthesis of Jiangxi Normal University;supported in part by a Grant-in-Aid for Scientific Research(C)(No.26460143)(AK)from the Japanese Society for the Promotion of Science(JSPS)

摘  要:A series of C-7 modified analogues of casuarine have been synthesized from sugar-derived nitrone and assayed against various glycosidases. Introduction of C-7 aminomethyl or amide group led to sharp decrease of the inhibitory activities.A series of C-7 modified analogues of casuarine have been synthesized from sugar-derived nitrone and assayed against various glycosidases. Introduction of C-7 aminomethyl or amide group led to sharp decrease of the inhibitory activities.

关 键 词:Nitrone 1.3-Dipolar cycloaddition Ammonolysis Glycosidase inhibitors Polyhydroxylated pyrrolizidines 

分 类 号:TQ464[化学工程—制药化工]

 

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