One-Step Synthesis of Phosphate-Based Inhibitors and Applications Thereof

摘要

One-step methods for forming phosphate-based enzyme inhibitors are disclosed. Methods include reacting o-phosphorylethanolamine with an acyl chloride at acidic conditions. Acyl chlorides can be derivatized. The phosphate-based enzyme inhibitors can inhibit enzymes of the pentose phosphate pathway including D-ribose-5-phosphate aldose-ketose isomerase enzymes such as T. cruzi ribose 5-phosphate isomerase type B and D-ribulose-5-phosphate 3-epimerase enzymes. Methods can be used in forming pharmaceutical compositions for use in treatment of disease caused by kinetoplastid parasites including T. cruzi, T. brucei, and Leishmania spp.