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Title: The search for histamine H3 and H4 receptor ligands

Abstract:

The aim of this work was to obtain novel, active histamine H3 and H4 receptor ligands.Compounds were obtained according the proposed schemes based on lead structures, 47 in total. All of the obtained histamine H3 receptor ligands fit to the general histamine H3 receptor core proposed by Lipp. This group of compounds could be divided in two subgroups: piperazine and piperidine derivatives. Also, highly active fluorescent histamine H3 receptor ligand was obtained, as well as (cyclic)thiourea derivatives with expected histamine H4 receptor activity.Compounds were obtained via traditional organic synthesis, as well as with the use of microwave irradiation. All of the obtained derivatives were then tested in vitro for desired histamine receptor activity. For the group of piperidine derivatives lipophilicity studies were provided, using reversed phase planar chromatography method. Experimental values were then compared with values obtained by various computational programs. Fluorescent properties of one of the compounds were also studied.Computational approaches, allowed the in silico visualization of binding to histamine H3 receptor model described by Levoin et al

Place of publishing:

Kraków

Level of degree:

2 - studia doktoranckie

Degree discipline:

chemia ; farmacja

Degree grantor:

Uniwersytet Jagielloński. Collegium Medicum. Wydział Farmaceutyczny. Katedra Technologii i Biotechnologii Środków Leczniczych.

Promoter:

Katarzyna Kieć-Kononowicz

Date issued:

2011

Identifier:

oai:dl.cm-uj.krakow.pl:3432

Call number:

ZB-116237

ControlNumberVIRTUA:

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Language:

pol ; eng

Access rights:

tylko w bibliotece

Location of original object:

Biblioteka Medyczna Uniwersytetu Jagiellońskiego- Collegium Medicum

Object collections:

Last modified:

Oct 18, 2019

In our library since:

Mar 6, 2013

Number of object content hits:

17

Number of object content views in PDF format

17

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/3432

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ZB-116237 Oct 18, 2019
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