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Ethynylphenyl carbonates and carbamates as dual-action acetylcholinesterase inhibitors and anti-inflammatory agents.

Abstract：

:Novel ethynylphenyl carbonates and carbamates containing carbon- and silicon-based choline mimics were synthesized from their respective phenol and aniline precursors and screened for anticholinesterase and anti-inflammatory activities. All molecules were micromolar inhibitors of acetylcholinesterase (AChE), with IC50s of 28-86 μM; the carbamates were two-fold more potent than the carbonates. Two of the most potent AChE inhibitors suppressed 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation by 40%. Furthermore, these molecules have physicochemical properties in the range of other CNS drugs. These molecules have the potential to treat inflammation; they could also dually target Alzheimer's disease through restoration of cholinergic balance and inflammation suppression.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Saxena J,Meloni D,Huang MT,Heck DE,Laskin JD,Heindel ND,Young SC

doi

10.1016/j.bmcl.2015.10.039

subject

Has Abstract

pub_date

2015-12-01 00:00:00

pages

5609-12

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)30148-7

journal_volume

25

pub_type

杂志文章

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