2,2-Dialkylnaphthalen-1-ones as new potassium channel activators
- 1 July 1993
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 36 (15) , 2121-2133
- https://doi.org/10.1021/jm00067a011
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.Keywords
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