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Phosphonamidate Compounds for Butyrylcholinesterase Selective Inhibitors
Author(s) -
Oh Jintaek,
Park JungYoul,
Park Kyoung Chan,
Hwang Ji Hyun,
Park Jeong Ho
Publication year - 2020
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.12126
Subject(s) - butyrylcholinesterase , acetylcholinesterase , aché , cholinesterase , galantamine , chemistry , cholinergic , stereochemistry , enzyme , combinatorial chemistry , organic chemistry , pharmacology , medicine , donepezil , dementia , disease
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 ± 0.02 μM for equine BuChE), whose IC 50 value was slightly lower than the IC 50 value of galantamine (IC 50 = 9.4 ± 2.50 for equine BuChE).