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Title: Structure - pharmacological activity relationship in aminopropan-2-ol derivatives
Abstract:
The aim of this work is to examine the relationship between the structure and affinity to adrenergic receptors antiarrhythmic and hypotcnsive activity within the group of 9 new derivatives of 2-aminopropanol as well as determining the pharmacological properties for the selected compound-(1-H-indol-4-yloxy)-3-{ [2-(2-methoxyphenoxy)ethylo] amino} propan-2-ol in the form of racemic mixture (R,S) and both enantiomers (R), (S) (synthesized in the Department of Industrial and Materials Chemistry, Rzeszow University of Technology). Pharmacological testing included: affinity to a.1-,a.2- and B1-adrenergic receptors, antiarrhythmic and hypotensive activity, influence on rat electrocardiogram in vivo and in vitro, influence on a pressor responses to epinephrine, norepincephrine and metoxamine, influence on smooth muscle of isolated rabbit small intestine, adrenolytic activity on isolated organs, influence on CNS, acute toxicity after i.v. and p.o. administration, influence on plasma oxidative state and blood glucose level as well as determining of basic pharmacokinetic parameters. Pharmacological testing revealed that compound (R,S)-9 and its enantiomers possessadrenolytic, antiarrhythmic and hypotensive activity and the strongest activity was observed for (S)-9. Moreover compound (R,S)-9 showed weak antioxidant activity and prevented the development of hyperglycemia induced by ; dexamethasone administration but did not influence spontaneous locomotor activity in mice. Pharmacokinetic tests showed stereoselective disposition of compound (R,S)-9 in rat plasma after i.v. administration. Analysis of obtained results showed that the substitution of carbazol moiety, present in carvedilol, for indole moiety did not deprive a new compound of its pharmacological activity and that B-adrenolytic activity, is mostly influenced by steric configuration of selected compound.
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Last modified:
Jul 20, 2022
In our library since:
Nov 21, 2012
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4
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http://dl.cm-uj.krakow.pl:8080/publication/1016
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| Edition name | Date |
|---|---|
| ZB-107974 | Jul 20, 2022 |
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