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Water-soluble betaines and amines based on thiacalix[4]arene scaffold as new cholinesterase inhibitors.

Abstract：

:Novel ammonium and betaine derivatives of p-tert-butylthiacalix[4]arene in cone and 1,3-alternate conformation were synthesized with high yields for the first time. The obtained compounds form in water spherical nanoparticles. It was shown by molecular docking calculations and in vitro experiments that amino and betaine derivatives can inhibit acetylcholinesterase and butyrylcholinesterase on the level of pyridostigmine while the toxicity of the obtained compounds is much lower than that of pyridostigmine.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Padnya PL,Bayarashov EE,Zueva IV,Lushchekina SV,Lenina OA,Evtugyn VG,Osin YN,Petrov KA,Stoikov II

doi

10.1016/j.bioorg.2019.103455

subject

Has Abstract

pub_date

2020-01-01 00:00:00

pages

103455

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)31452-X

journal_volume

94

pub_type

杂志文章

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