Synthesis and Biological Evaluation of 5′‐Triazole Nucleosides

摘要: The first series of 5'-triazole cytidines la-d and adenosines 2a-c was prepared evaluated for inhibitory potency toward a-2,3-sialyltransferase. synthesis target compounds achieved by converting the 5'-alcohol protected nucleosides to azide derivatives, which were then coupled with alkynes copper(I)-catalyzed cycloaddition give 3a-d/7a-c, followed deprotection. 5'-Triazole less efficient inhibitors α-2,3-sialyltrans-ferase than their cytidine analogues la-d. 1d most active compound an IC 50 37.5 uM. These results suggested that hydrophobic functionality group are clearly required improved binding.