In:
Bulletin of the Korean Chemical Society, Wiley, Vol. 40, No. 6 ( 2019-06), p. 544-553
Abstract:
Tryptamine–triazole hybrid compounds ( 11 – 18 ) were synthesized via click reaction between tryptamine azide and propargylated natural compounds. Their cholinesterase inhibitory activity was evaluated. Among the eight compounds, compound 11 showed the most potent inhibitory activity [IC 50 = 0.42 ± 0.29 μM for equine butyrylcholinesterase (BuChE) and 1.96 ± 0.15 μM for human BuChE]. From the molecular modeling study, compound 11 was bound to the catalytic anionic site, anionic subsite, peripheral anionic subsite, acyl‐binding pocket, and oxyanion hole of human or horse BuChE by forming a hairpin or U‐shaped structure. The Lineweaver‐Burk plot of compound 11 against BuChE suggests a mixed type of inhibition which corresponds well with the molecular modeling study.
Type of Medium:
Online Resource
ISSN:
1229-5949
,
1229-5949
DOI:
10.1002/bkcs.2019.40.issue-6
Language:
English
Publisher:
Wiley
Publication Date:
2019
detail.hit.zdb_id:
2056474-0
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