Abstract
A series of 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazoles is described. The compounds were investigated in vitro for beta-adrenoceptor antagonism, and several examples were found to be selective for the beta 1-adrenoceptor. The structure--activity relationship exhibited by this series of compounds is discussed. (S)-2-[p-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-2-hydroxypropoxy]phenyl]-4-(2 -thienyl)imidazole [(S)-13] was over 100 times more selective than atenolol for the beta 1-adrenergic receptor and has been selected for in-depth studies.
MeSH terms
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Adrenergic alpha-Agonists / chemical synthesis*
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Animals
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Female
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Guinea Pigs
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Heart / drug effects
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Heart / physiology
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology
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Indicators and Reagents
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Isoproterenol / pharmacology
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Magnetic Resonance Spectroscopy
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Receptors, Adrenergic / chemical synthesis*
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Receptors, Adrenergic, beta / chemical synthesis*
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Receptors, Adrenergic, beta / pharmacology
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Structure-Activity Relationship
Substances
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Adrenergic alpha-Agonists
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Imidazoles
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Indicators and Reagents
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Receptors, Adrenergic
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Receptors, Adrenergic, beta
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Isoproterenol