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

Title: The search for non-imidazole histamine H3-receptor antagonists

Abstract:

The aim of this work was the synthesis of new compounds with expected antagonistic histamine H3 receptor activity. The introduction of the work described the newest information about histamine H3 receptors. In the chemical part there are described structures of compounds with the way of their synthesis. Two different types of products were prepared: carbamates (44 compounds) and ethers (36 compounds). Their purity and structures were confirmed by standard spectral techniques (1H-NMR, MS, IR) and elemental analysis. The novel compounds were investigated as antagonists for their activity at histamine H3 receptors both in vitro and in vivo Additionally, the carbamates were tested for their histamine H1- and H2-receptors activity and muscarine M3 receptors affinity. For the most active structures in silico methods were used to predict their metabolism. Three different computer programmes were examined (Metabo/Expert, Meteor and MetaSite). The results are presented on Figures and discussed. Lipophilicity for selected compounds (aliphatic carbamates) was determined by reversed-phase thin-layer chromatography (RP-TLC). The partition coefficient logP was also calculated by means of computer programmes (HyperChem, ClogP, Meteor, Pallas and ScilogP). Penetration across blood-brain barrier was predicted for selected carbamates and ethers using simple rules (described in the literature) an ; d computer programme Absolv (logBB).

Place of publishing:

Kraków

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmacja

Degree grantor:

Wydział Farmaceutyczny

Promoter:

Kieć-Kononowicz, Katarzyna

Date issued:

2004

Identifier:

oai:dl.cm-uj.krakow.pl:1275

Call number:

ZB-100259

Language:

pol

Access rights:

tylko w bibliotece

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Last modified:

Jul 18, 2022

In our library since:

Nov 21, 2012

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16

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0

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/1275

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