Abstract
A series of compounds 1b-f, 2b-f, and 3b-f having an o-chlorobenzenesulfonamidic diuretic moiety variously linked to the nitrogen side chain of the beta-blocking (aryloxy)propanolamine pharmacophore were prepared and tested for their beta 1-adrenoceptor affinity. For all the active compounds, beta-blocking and diuretic activities were investigated in rats; the structure--activity relationships are discussed. Some of the compounds displayed varying levels of both properties and among these, compounds 1c and 2c have been chosen for further development.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic beta-Antagonists / chemical synthesis*
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Adrenergic beta-Antagonists / chemistry
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Adrenergic beta-Antagonists / pharmacology
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Animals
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Binding Sites / drug effects
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Diuretics / chemical synthesis*
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Male
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Propanolamines / chemical synthesis*
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Propanolamines / chemistry
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Propanolamines / pharmacology
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Rats
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Rats, Wistar
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacology
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Turkeys
Substances
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Adrenergic beta-Antagonists
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Diuretics
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Propanolamines
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Sulfonamides