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

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

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Praca doktorska

Abstract:

The PhD thesis focuses on structural factors determining selectivity of arylpiperazine and arylsulfonamide derivatives for 5-HTlA and 5-HT7 receptors. The synthesis and SAR analysis of pyrrolidine and benzotriazole derivatives confirmed that linearly extended conformation of LCAP is bioactive for 5-HTlA receptors, whereas this geometry is unfavorable for the 5-HT7 receptors. In the group of benzisoxazolepiperazine derivatives the use of sulfonamide fragment, additionally rigidified by the piperidine ring, is significant for high affinity for 5-HT7R; however, the activity toward 5-HT1AR (and others monoaminergic receptors) is not completely eliminated. It was found, that the lack of aromatic groups m the vicinity of protonated nitrogen atom (perhydroisoquinoline derivatives) is essential for selectivity to 5-HT7R vs 5-HT1AR. Docking studies showed that these ligands are located between helices 3, 6 and 7, within the so-called selective part of 5-HT7R binding pocket. Moreover, based on new arylsulfonamide derivatives the 3D QSAR pharmacophore model was generated. It extends the previous selectivity hypothesis (obtained in structure-based approach), by defining the additional hydrophobic region, located near aromatic feature.

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Level of degree:

2 - studia doktoranckie

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Degree grantor:

Wydział Farmaceutyczny

Promoter:

Bojarski, Andrzej J.

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Identifier:

oai:dl.cm-uj.krakow.pl:760

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Subject and keywords:

5-HT7 5-HT1A receptors serotonin ligands

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Digital Medical Library > PhD thesis database

Last modified:

Jun 26, 2023

In our library since:

Nov 21, 2012

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1 116

Number of object content views in PDF format

229

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http://dl.cm-uj.krakow.pl:8080/publication/760

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Edition name	Date
ZB-111670	Jun 26, 2023

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