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Triazole-Linked Iminosugars and Aromatic Systems as Simplified UDP-Galf Mimics: Synthesis and Preliminary Evaluation as Galf-Transferase Inhibitors
European Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2017-11-06 05:26:23 , DOI: 10.1002/ejoc.201701283
Chloé Cocaud 1 , Audrey Maujoin 1 , Ruixiang B. Zheng 2 , Todd L. Lowary 2 , Nuno Rodrigues 1 , Nathalie Percina 1 , Agnes Chartier 1 , Frédéric Buron 1 , Sylvain Routier 1 , Cyril Nicolas 1 , Olivier R. Martin 1
Affiliation  

The convenient preparation of 1-C-propargyl-imino-l-arabinitol derivatives coupled by a triazole tether to various aromatic and heteroaromatic groups is reported. These structures, which can be considered to be simplified mimics of UDP-Galf, the substrate of GlfT2, a galactofuranosyltransferase present in mycobacteria, were evaluated as inhibitors of the enzyme and were found to have significant activity.

中文翻译:

三唑连接的氨基糖和芳香系统作为简化的UDP-半乳糖模拟物:合成和初步评估作为半乳糖转移酶抑制剂。

已经报道了通过三唑系链与各种芳族和杂芳族基团偶联的1 - C-炔丙基-亚氨基-1-阿拉伯糖醇衍生物的方便制备。这些结构中,其可以被认为是简化的UDP-Gal的模拟物˚F,GlfT2,存在于分枝杆菌galactofuranosyltransferase的基板,进行评价作为酶的抑制剂,并发现有显著活性。
更新日期:2017-11-06
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