Abstract
A series of 3-amino-1-(5,6,7,8-tetrahydronaphthoxy)-2-propanols was synthesized and investigated for beta-adrenergic blocking activity and direct myocardial depressant action. The cis- and trans-diols 12--15 were found to retain the beta-blocking potency of propranolol but to lack its myocardial depressant action. Compound 15 (nadolol) is currently undergoing extensive clinical evaluation as a potential antianginal, antiarrhythmic, and antihypertensive agent.
MeSH terms
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Adrenergic beta-Antagonists / chemical synthesis*
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Adrenergic beta-Antagonists / pharmacology
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Animals
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Cats
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Epoxy Compounds
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Guinea Pigs
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In Vitro Techniques
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Isoproterenol / antagonists & inhibitors
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Methods
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Myocardial Contraction / drug effects
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Phenols
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Propanolamines / chemical synthesis*
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Propanolamines / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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Adrenergic beta-Antagonists
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Epoxy Compounds
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Phenols
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Propanolamines
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Isoproterenol