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Title: The search for histamine H3 and H4 receptor ligands


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

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Level of degree:

2 - studia doktoranckie

Degree discipline:

chemia ; farmacja

Degree grantor:

Wydział Farmaceutyczny


Kieć-Kononowicz, Katarzyna

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pol; eng

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tylko w bibliotece

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Last modified:

Mar 17, 2023

In our library since:

Mar 6, 2013

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Edition name Date
ZB-116237 Mar 17, 2023


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