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Title: Pyridinylpiperazine derivatives as 5-HT6 antagonists that affect central nervous system

Author:

Olszak-Płachta, Marta

Date:

2023

Type:

Praca doktorska

Abstract:

5-HT6 receptors are mainly located in the central nervous system. It has been shown that block-ade of 5-HT6R increases acetylcholine and glutamate level. Acetylcholine and glutamate are neu-rotrasmitters involved in cognitive functions, learning processes, concentrations and memory. The aim of the thesis focuses on synthesis of a new pyridylpiperazine derivatives as a 5-HT6 re-ceptor antagonists that affect central nervous system. Design of compounds based on the four key structural elements for 5-HT6 antagonism: a positive ionizable atom, an aromatic ring, a hy-drogen bond acceptor group, and hydrophobic site. The crucial step of synthesis was Katrizkys Reaction – the formation of the pyridine ring in a one pot process involving the reaction of α,β unsaturated ketones, amines and 1H-benzotriazole-1-acetonitrile. Final free base compounds were converted into HCl or fumaric acid salt. Research allowed to find new very potent and se-lective 5-HT6 receptor antagonist: 1-[4-(4-methoxyphenyl)-6-(oxan-4-ylmethyl)pyridin-2-yl]-4-methylpiperazine (98). This new pyridylpiperazine derivative with very high blood-brain barier permeability, good results for cytochrome P450 inhibition might determine promising strategy for further development in treatment of CNS deseases.

Place of publishing:

Kraków

Level of degree:

2 - studia doktoranckie

Degree grantor:

Rada Dyscypliny Nauki farmaceutyczne

Promoter:

Bojarski, Andrzej J.

Date issued:

2022

Identifier:

oai:dl.cm-uj.krakow.pl:5069

Call number:

ZB-139444

Language:

pol

Access rights:

tylko w bibliotece

Subject and keywords:

5-HT 6 R antagonist Katritzkis Reaction pyridinylpiperazine serotonin

Object collections:

Last modified:

Apr 8, 2024

In our library since:

Apr 8, 2024

Number of object content hits:

10

Number of object content views in PDF format

0

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/5070

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Edition name Date
ZB-139444 Apr 8, 2024

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