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

Article abstract of DOI:10.1021/jm00067a011

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-oxonaphthalene-6-carbonitrile, 17f (UR-8225), has been selected for further pharmacological development.