Phosphonamidate Compounds for Butyrylcholinesterase Selective Inhibitors

摘要

To find a new type of cholinergic drug, phosphonamidate compounds 18–32 were synthesized using a click reaction between propargylated‐9,10‐Dihydro‐9‐oxa‐10‐phosphaphenanthrene‐10‐oxide (DOPO, 2) and substituted benzyl azide. Their inhibitory activity against butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE) was evaluated. Compound 31 was the most active of the 15 compounds (IC50 = 3.14?±?0.02?μM for equine BuChE), whose IC50 value was slightly lower than the IC50 value of galantamine (IC50 = 9.4?±?2.50 for equine BuChE).