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

DOI: 10.1021/jm00067a011

Source and publish data:

Journal of Medicinal Chemistry p. 2121 - 2133 (1993)

Update date:2022-07-30

Topics:

Authors:

Almansa Almansa

Gomez Gomez

Cavalcanti

Rodriguez

Carceller

Bartroli

Garcia-Rafanell

Forn Forn

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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.

Full text of DOI:10.1021/jm00067a011

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