Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT6 receptor with anti-aggregation properties against amyloid-beta and tau.
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Wichur T, et al.
Eur J Med Chem. 2021 Dec 5;225:113783. doi: 10.1016/j.ejmech.2021.113783. Epub 2021 Aug 19.
Eur J Med Chem. 2021.
PMID: 34461507
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Compound 17, a tacrine derivative is a reversible inhibitor of acetyl- and butyrylcholinesterase (IC(50) = 8 nM and IC(50) = 24 nM respectively), while compound 35 with rivastigmine-derived phenyl N-ethyl-N-methylcarbamate fragment is a selective, pseudo-irre …
Compound 17, a tacrine derivative is a reversible inhibitor of acetyl- and butyrylcholinesterase (IC(50) = 8 nM and IC(50) = 24 nM respectiv …