Abstract
The synthesis of (2RS)-1-(5-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and (2RS)-1-(7-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and its enantiomers, analogs of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol ((RS)-9) is described. Compounds were tested for electrographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for alpha(1)-, alpha(2)- and beta(1)-adrenoceptors binding affinities. The antagonist potency of the new compounds was compared with carvedilol and (RS)-9.
MeSH terms
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2-Propanol / chemical synthesis*
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2-Propanol / chemistry
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2-Propanol / pharmacology
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Adrenergic Antagonists / chemical synthesis*
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Adrenergic Antagonists / chemistry
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Animals
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Antihypertensive Agents / chemical synthesis*
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Antihypertensive Agents / chemistry
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Antihypertensive Agents / pharmacology
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Carbazoles / chemical synthesis*
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Carbazoles / chemistry
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Carbazoles / pharmacology
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Carvedilol
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Ileum / drug effects
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Male
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Molecular Structure
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Propanolamines / chemical synthesis*
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Propanolamines / chemistry
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Propanolamines / pharmacology
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Rabbits
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Rats
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Rats, Wistar
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Stereoisomerism
Substances
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Adrenergic Antagonists
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Antihypertensive Agents
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Carbazoles
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Propanolamines
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Carvedilol
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2-Propanol