Novel anilide and benzylamide derivatives as 5-HT1A/5- HT7 receptor ligands and phosphodiesterase type 4 and 7 inhibitors with potential procognitive and antidepressant activity - Digital Medical Library

Skip to main menu
Skip to search engine
Skip to content
Skip to footer

Download

This publication is protected and can be accessed only from certain IPs.

This publication is protected and can be accessed only from certain IPs.

Description
Information

Title: Novel anilide and benzylamide derivatives as 5-HT1A/5- HT7 receptor ligands and phosphodiesterase type 4 and 7 inhibitors with potential procognitive and antidepressant activity

Author:

Jankowska, Agnieszka Wioleta

Date:

Type:

Praca doktorska

Abstract:

The search for drugs for the treatment of memory and mood disorders belongs to one of the leading research topics worldwide. The aim of the thesis was to design and synthesize novel anilide and benzylamide derivatives of long-chain cyclic amines as multifunctional ligands of serotonin 5-HT1A and 5-HT7 receptors as well as phosphodiesterase (POE) 4 and 7 inhibitors with potentia! procognitive and antidepressant properties. A series of 90 designed compounds was obtained by using classical organie chemistry methods. The synthesized derivatives were potent-to-weak 5-HT1A and 5-HT7 receptors ligands. Many of them showed features of PDE4B and/or PDE7A inhibitors. On the basis of the obtained in vitro results, structure- activity relationship studies were performed. In vitro functional tests enabled to select potent 5-HT1A receptor antagonists with various 5-HT7 receptor antagonistic properties. In vitro ADME studies allowed to select high-permeable compounds with improved metabolic stability. The most promising derivatives showed procognitive and antidepressant properties in vivo. Finally, neuroprotective properties in vitro were demonstrated for the representative compounds. Research results suggest that the simultaneous interaction with 5- HT 1A and 5-HT7 receptors and PDE4B and/or PDE7A inhibition may be a promising strategy for treating cognitive and depressive disorders.

Place of publishing:

Level of degree:

2 - studia doktoranckie

Degree discipline:

Degree grantor:

Rada Dyscypliny Nauki farmaceutyczne

Promoter:

Chłoń-Rzepa, Grażyna

Date issued:

Identifier:

oai:dl.cm-uj.krakow.pl:4593

Call number:

Language:

Access rights:

tylko w bibliotece

Subject and keywords:

cognitive and depressive disorders multifunctional ligands PDE4 and PDE7 inhibitors 5-HT1A and 5-HT7 receptors ligands procognitive and antidepressant activity

Object collections:

Digital Medical Library > PhD thesis database

Last modified:

Apr 30, 2024

In our library since:

Mar 31, 2022

Number of object content hits:

11

Number of object content views in PDF format

0

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/4594

Show description in RDF format:

Show description in OAI-PMH format:

Edition name	Date
ZB-134218	Apr 30, 2024

Objects

Similar

Novel anilide and benzylamide derivatives as 5-HT1A/5- HT7 receptor ligands and phosphodiesterase type 4 and 7 inhibitors with potential procognitive and antidepressant activity

Jankowska, Agnieszka Wioleta

2021

Praca doktorska

Structural modifications of arylpiperazine and arylsulfonamide serotonin 5-HT1A and 5-HT7 receptor ligands in search of factors determining selectivity

Bugno, Ryszard

2010

Praca doktorska

Chemical and pharmacological studies in group of 3,3-disubstituted derivatives of pyrrolidyne-2,5-dion with potential anticonvulsant activity

Chlebek, Iwona

2013

Praca doktorska

Novel aryl-alkyl-piperazines with N-acylated amino acids as serotoninergic receptors ligands

Zajdel, Paweł

2006

Praca doktorska

The cellular mechanisms underlying the fast antidepressant-like and procognitive effects of HBK-15

Sałaciak, Kinga

2022

Praca doktorska

Synthesis and characterization of novel multifunctional ligands aiming at symptoms and causes of Alzheimer's disease

Wichur, Tomasz

2020

Praca doktorska

Working memory disturbances in patients with major depression after ECT treatment

Datka, Wojciech

2009

Praca doktorska

Synthesis and Biological Evaluation of New Donepezil-based Benzylamine Derivatives As Multiple Ligands Targeting Cholinesterases and Amyloid Beta

Szałaj, Natalia

2015

Praca doktorska

More

Citation style:

Contact details

Address

Medical Library
Medyczna 7
30-688 Krakow

Phone

12 658 72 56
517 385 669

E-Mail

Collecting and Elaboration Department
cyfrowabm@cm-uj.krakow.pl

Visit us!

https://bm.cm.uj.edu.pl/en/main-page/

This page uses 'cookies'. More information