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2,2-Dialkylnaphthalen-1-ones as new potassium channel activators.

Authors :
Almansa C
Gómez LA
Cavalcanti FL
Rodríguez R
Carceller E
Bartrolí J
García-Rafanell J
Forn J
Source :
Journal of medicinal chemistry [J Med Chem] 1993 Jul 23; Vol. 36 (15), pp. 2121-33.
Publication Year :
1993

Abstract

A new series of 2,2-dialkylnaphthalen-1-one potassium channel activators has been prepared, and their in vitro relaxant activities in isolated rat portal vein and guinea pig tracheal spirals as well as their oral antihypertensive effect in spontaneously hypertensive rats have been evaluated. The group of 1,2-dihydro-4-(1,2-dihydro-2-oxo-1-pyridyl)-2,2-dimethylnaphthalen -1- ones with an electron-withdrawing substituent at the 6-position contain the most active compounds and 1,2-dihydro-4-(1,2-dihydro-2-oxo-1-pyridyl)-2,2-dimethyl-1-oxonaphtha lene-6- carbonitrile, 17f (UR-8225), has been selected for further pharmacological development.

Details

Language :
English
ISSN :
0022-2623
Volume :
36
Issue :
15
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
8340916
Full Text :
https://doi.org/10.1021/jm00067a011