o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.
Article Details
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Cecchetti V, Fravolini A, Schiaffella F, Tabarrini O, Bruni G, Segre G
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.
J Med Chem. 1993 Jan 8;36(1):157-61.
- PubMed ID
- 8093626 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Carteolol Beta-1 adrenergic receptor Ki (nM) 1.9 N/A N/A Details Propranolol Beta-1 adrenergic receptor Ki (nM) 2.3 N/A N/A Details