New glucocerebrosidase inhibitors by exploration of chemical diversity of N-substituted aminocyclitols using click chemistry and in situ screening

L Díaz, J Casas, J Bujons, A Llebaria…

文献索引：Diaz, Lucia; Bujons, Jordi; Casas, Josefina; Llebaria, Amadeu; Delgado, Antonio Journal of Medicinal Chemistry, 2010 , vol. 53, # 14 p. 5248 - 5255

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被引用次数: 31

摘要

A library of aminocyclitols derived from CuAAC reaction between N-propargylaminocyclitol 4 and a series of azides [1− 25] is described and tested against GCase. Azides have been chosen from a large collection of potential candidates that has been filtered according to physical and reactivity constraints. A synthetic methodology has been optimized in order to avoid the use of protecting groups on the aminocyclitol scaffold. Because the reaction can ...