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Title: Affinity for adrenergic receptors and pharmacological activity of 7,8-disubstituted teophylline analogs
Abstract:
Searching for compounds with potential activity on cardiovascular system within the group of 7,8- disubstituted derivatives of theophylline m the Department of Pharmaceutical Chemistry of Collegium Medicum of Jagiellonian University, we obtained new 7-β-hydroxy- γ-(N4phenoxyethylpiperazine)-propyl derivatives. Initial pharmacological studies lead to the selection of 7- β -hydroxy- γ -(N4-phenoxyethylpiperazine)-propyltheophylline dihydrochloride (CH-1), a compound that exhibits an antiarrythmic, hypotensive activity and an affinity for α1, and α2 -adrenergic receptors. As a result of a modification of the compound CH-1 consisting in the introduction of vanous arylalkylamino or aminoalkylamino substituents at the 8-position of theophylline, as well as, by substituting phenoxyethylpiperazine by another piperazine group, seven active structures were obtained that exhibited comparable or higher antiarrythmic and/or hypotensive effect and the affinity for α1 and α2-adrenergic receptors than CH-1 . The studies carried out allow us to state that the highest affinity for α1-adrenergic receptors is demonstrated by compounds having a phenoxyethylpiperazine or phenylpiperazine group in their structure. The most advantageous for the antiarrythmic activity is the presence of the phenoxyethylpiperazine or phenylpiperazine group at the 7-position of theophylline, and the 2-morpholineethylamin ; o substituent at the 8-position. For hypotensive activity, however, the most advantageous is the presence of the phenoxyethylpiperazine group at the 7-position of theophylline, and the 2-benzylamino- or 2-pyridylmethylamino substituent at the 8-position. Hypotensive effect of the studied compounds most probably results from their α-adrenolytic and spasmolytic activity, whereas the antiarrythmic activity in the model of adrenaline arrythmia results from blocking α-adrenergic receptors.
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Last modified:
Feb 12, 2024
In our library since:
Nov 21, 2012
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874
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All available object's versions:
http://dl.cm-uj.krakow.pl:8080/publication/1243
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| Edition name | Date |
|---|---|
| ZB-102637 | Feb 12, 2024 |
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