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Title: Pharmacological research of selected piperazine derivatives with potential cardiovascular activity
Abstract:
The influence of 8 piperazine derivatives on the cardiovascular system was evaluated and their mechanism of action and structure activity relationship was explained in the thesis. In the preliminary pharmacological screening the six active aroxyalkyl derivatives of 2-methoxyphenylpiperazine or phenoxyethylpiperazine with high hypotensive and antiarrhythmic activity were selected. Their influence on circulation appeared to be connected with the interaction with 4 types of G-protein coupled receptors: a1i-, a2-adrenergic and 5-HT1A, 5-HT2A-serotoninergic ones. The two most active compounds: 1-(3-(2,6-dimethylphenoxy)propyl-4-(2- methoxyphenyljpiperazine hydrochloride (compound 2) and 1-(3-(2-chloro-6-methyIophenoxy)propyl)-4-(2- methoxyphenyljpiperazine hydrochloride (compound 5) showed the highest affinity and selectivity for a1- adrenoceptors. They turned out to be the competitive antagonists of a1-adrenoceptors with stronger activity at a1D, a1A and a1L and weaker at a1B subtype of a1-adrenoceptors. The study of the structure activity relationship indicated that the key structure element determinig a1-adrenolytic activity was 2-methoxyphenylpiperazine moiety connected with phenoxyl group by propyl chain, as well as the presence of the substituents at ortho position (2 and/or 6) in phenoxyl group. Both the shortening of the propyl chain and the presence of the substituent at ; meta position in phenoxyl group decreased the affinity and seletivity for a1-adrenergic receptors. The exchange of phenypiperazine moiety into the second phenoxyalkylpiperazine group decreased the affinity for a- adrenergic and serotoninergic receptors.
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Last modified:
Mar 10, 2023
In our library since:
Nov 21, 2012
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33
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All available object's versions:
http://dl.cm-uj.krakow.pl:8080/publication/776
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| Edition name | Date |
|---|---|
| ZB-111785 | Mar 10, 2023 |
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