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nleslie321
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Location: krakatoa
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Mood: just right
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Im going to try give it a go this weekend.
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solo
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Mood: ....getting old and drowning in a sea of knowledge
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Reference Information
Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with b-amyloid anti-aggregation properties and beneficial effects
on memory in vivo
Anna Wie˛ckowska
Bioorg. Med. Chem.
23 (2015) 2445–2457
Abstract
Due to the complex nature of Alzheimer’s disease, multi-target-directed ligand approaches are one of the
most promising strategies in the search for effective treatments. Acetylcholinesterase, butyrylcholinesterase
and b-amyloid are the predominant biological targets in the search for new anti-
Alzheimer’s agents. Our aim was to combine both anticholinesterase and b-amyloid anti-aggregation
activities in one molecule, and to determine the therapeutic potential in vivo. We designed and synthesized
28 new compounds as derivatives of donepezil that contain the N-benzylpiperidine moiety combined
with the phthalimide or indole moieties. Most of these test compounds showed micromolar
activities against cholinesterases and aggregation of b-amyloid, combined with positive results in
blood–brain barrier permeability assays. The most promising compound 23 (2-(8-(1-(3-chlorobenzyl)
piperidin-4-ylamino)octyl)isoindoline-1,3-dione) is an inhibitor of butyrylcholinesterase
(IC50 = 0.72 lM) that has b-amyloid anti-aggregation activity (72.5% inhibition at 10 lM) and can cross
the blood–brain barrier. Moreover, in an animal model of memory impairment induced by scopolamine,
the activity of 23 was comparable to that of donepezil. The selected compound 23 is an excellent lead
structure in the further search for new anti-Alzheimer’s agents.
Note...see scheme 1
Unable to upload the article...
https://www.sciencedirect.com.sci-hub.tw/science/article/pii...
[Edited on 26-2-2020 by solo]
It's better to die on your feet, than live on your knees....Emiliano Zapata.
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nleslie321
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So I finally got the debenzylation to work using 10% Pd/C in an acetic environment. Thanks for everyone who helped me out.
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spankyetal
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Quote: Originally posted by nleslie321  | Yes i did that exact reaction you linked. The N-benzyl-4-piperidone is from sigma and other chemicals all bought from well known chemical supply
companies. Heres the paper-
"Synthesis and biological evaluation of some novel 1-substituted fentanyl analogs in Swiss albino mice" Shiv Kumar YADAV,
Chandra Kant MAURYA, Pradeep Kumar GUPTA, Ajai Kumar JAIN, Kumaran GANESAN, Rahul BHATTACHARYA. |
No such animal from the piperidine family that doesn't destroy lives. The fentanyls only get abused the minute they are made. human nature being what
it is. China was, until mid 2019, supplying immediate precursors i.e., anilino precursors for about $1 usd per/gram. YUP $20 usd would get you 20
grams. So many packages sailing thru customs, a tsunami actually.
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