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- Title
Phosphonamidate Compounds for Butyrylcholinesterase Selective Inhibitors.
- Authors
Oh, Jintaek; Park, Jung‐Youl; Park, Kyoung Chan; Hwang, Ji Hyun; Park, Jeong Ho
- Abstract
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).
- Subjects
BUTYRYLCHOLINESTERASE; PARASYMPATHOMIMETIC agents; GALANTHAMINE; TACRINE; STRUCTURE-activity relationships; ACETYLCHOLINESTERASE
- Publication
Bulletin of the Korean Chemical Society, 2020, Vol 41, Issue 12, p1153
- ISSN
0253-2964
- Publication type
Article
- DOI
10.1002/bkcs.12126