o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.

Article Details

Citation

Copy to clipboard

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