[p-[(Thienylcarbonyl)amino]phenoxy]propanolamines derivatives as diuretic and β-adrenergic receptor blocking agents

The synthesis of [[(thienylcarbonyl)amino]phenoxy]propanolamines and their beta-adrenergic blocking and diuretic activity are described. Structure-activity relationships demonstrated that ortho substitution of the phenoxy ring with an hydrogen or an ester function leads to compounds possessing both...

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Veröffentlicht in:	Journal of medicinal chemistry 1986, Vol.29 (1), p.100-103
Hauptverfasser:	BOULEY, E, TEULON, J.-M, CAZES, M, CLOAREC, A, DEGHENGHI, R
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Blood Pressure - drug effects Chemical Phenomena Chemistry Diuresis - drug effects Dogs Exact sciences and technology Female Heart Rate - drug effects Heterocyclic compounds Heterocyclic compounds with o, s, se, te hetero atom and condensed derivatives Male Myocardial Contraction - drug effects Organic chemistry Preparations and properties Propanolamines - chemical synthesis Propanolamines - pharmacology Rats Rats, Inbred Strains Receptors, Adrenergic, beta - drug effects Receptors, Adrenergic, beta - physiology Structure-Activity Relationship
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Zusammenfassung:	The synthesis of [[(thienylcarbonyl)amino]phenoxy]propanolamines and their beta-adrenergic blocking and diuretic activity are described. Structure-activity relationships demonstrated that ortho substitution of the phenoxy ring with an hydrogen or an ester function leads to compounds possessing both activities. Ethyl 2-[3-[(1,1-dimethylethyl) amino]-2-hydroxypropoxy]-5-[(2-thienylcarbonyl)amino]benzoate (3d) was selected as the most active compound for further investigation.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00151a017