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Title: Synthesis and studies of reaction products of oxirane derivatives with heterocycles containing −NH−(C=)−Br functionality as potential cardiovascular agents

Author:

Baran, Marzena

Date:

2013

Type:

Praca doktorska

Abstract:

The purpose of the work was to explain the reaction mechanism of oxirane derivatives with heteroaromatic compounds containing −NH−(C=)−Br functionality and to synthesize new benzimidazole and pyridin-2-one derivatives as potential cardiovascular agents. The reactions of 2-bromobenzimidazole, 2-bromo-5-chlorobenzimidazole or 6-bromopyridin-2(1H)-one as the starting heterocyclic compounds with the aminomethyloxiranes were performed. The following amines: indoline, morpholine, and N-phenylpiperazine derivatives were chosen. The final products contained oxazole ring fused to an appropriate heterocyclic compound. The cyclic amide pyridin-2(1H)-one is subjected to lactam-lactim tautomerism, whereby an additional product containing 2-hydroxypropoxy fragment was formed. For the final compounds, pharmacological tests were performed to determine their inhibition of the phosphodiesterase activity, the affinity towards adrenergic and serotoninergic receptors. Additionally, anti/mutagenic and hypotensive activity for selected compounds with the best α1-adrenoceptor affinity (Ki < 160 nM) was tested. The results have shown that the studied compounds characterized antimutagenic properties in the Vibrio harveyi test and hypotensive activity in normotensive rats. Furthermore, the lipophilicity of the investigated compounds was assessed experimentally and in silico.

Place of publishing:

Kraków

Level of degree:

2 - studia doktoranckie

Degree discipline:

farmacja ; chemia ; farmakologia

Degree grantor:

Wydział Farmaceutyczny

Promoter:

Cegła, Marek

Date issued:

2013

Identifier:

oai:dl.cm-uj.krakow.pl:3629

Call number:

ZB-118805

Language:

pol; eng

Access rights:

tylko w bibliotece

Subject and keywords:

N-arylpiperazine derivatives pyridin-2(1H)-one alfa1-adrenoceptors benzimidazole phosphodiesterase

Object collections:

Last modified:

Mar 17, 2023

In our library since:

Nov 7, 2013

Number of object content hits:

23

Number of object content views in PDF format

0

All available object's versions:

http://dl.cm-uj.krakow.pl:8080/publication/3629

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Edition name Date
ZB-118805 Mar 17, 2023

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