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 (IC 50 = 3.14 AE 0.02 μM for equine BuChE), whose IC 50 value was slightly lower than the IC 50 value of galantamine (IC 50 = 9.4 AE 2.50 for equine BuChE).
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