A convenient and scalable synthesis of DGJNAc ID from D-glucuronolactone in an overall yield of 20% is provided. DGJNAc is the first highly potent and specific competitive inhibitor of GalNAcases. DGJNAc ID is also a competitive inhibitor of -hexosaminidases. Synthesis and activity of L-DGJNAc IL is also shown. The use of DGJNAc as a potent and specific inhibitor of GalNAcases will allow useful investigation and treatment of a number of diseases, including Schindler Disease.
提供了一种方便且可扩展的合成方法,从
D-葡萄糖醛酸内酯中合成DGJNAc ID,总收率为20%。DGJNAc是第一种高效而特异的竞争性GalNAcases
抑制剂。DGJNAc ID也是-hexosaminidases的竞争性
抑制剂。还展示了L-DGJNAc IL的合成和活性。将DGJNAc用作GalNAcases的高效而特异的
抑制剂,将允许对许多疾病进行有用的研究和治疗,包括Schindler病。