2,2-Dialkylnaphthalen-1-ones as new potassium channel activators.
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.
Almansa
C
C
Chemistry Laboratories, J. Uriach & Cía S. A., Barcelona, Spain.
Gómez
L A
LA
Cavalcanti
F L
FL
Rodríguez
R
R
Carceller
E
E
Bartrolí
J
J
García-Rafanell
J
J
Forn
J
J
D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D001578:Benzopyrans / Q000138:chemical synthesis* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D006168:Guinea Pigs; D008297:Male; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D015221:Potassium Channels / Q000187:drug effects*; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011918:Rats, Inbred SHR; D013329:Structure-Activity Relationship; D014132:Trachea / Q000187:drug effects
D000959:Antihypertensive Agents; D001578:Benzopyrans; D009281:Naphthalenes; D015221:Potassium Channels; D011728:Pyridones; C082407:UR 8225