149456-17-7Relevant academic research and scientific papers
2,2-Dialkylnaphthalen-1-ones as new potassium channel activators
Almansa,Gomez,Cavalcanti,Rodriguez,Carceller,Bartroli,Garcia-Rafanell,Forn
, p. 2121 - 2133 (2007/10/02)
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.
Tetralones with pharmacological activity
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, (2008/06/13)
The present invention relates to new tetralones having the formula I: STR1 wherein: R1 and R2 represent hydrogen, halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, pentafluoroethyl, ethynyl, trimethylsilylethynyl, C1-4 alkylcarbonylamino being the amino optionally substituted by a C1-4 alkyl group; R3 is hydrogen or C1-4 alkyl, and R4 is C1-4 alkyl, or R3 and R4 together form a C2-5 polymethylene chain; either R5 represents hydroxyl, acetoxy or formyloxy and R6 and R7 are both hydrogen, or R5 together with R6 form a carbonyl group and R7 is hydrogen, or R5 and R7 together form a bond and R6 is hydrogen; R8 is, among others, 1,2-dihydro-2-oxo-1-pyridyl, 2,3-dihydro-1-oxo-1H-isoindol-2-yl, 2-oxo-1-pyrrolidinyl, 2-oxo-1-pyperidinyl. The invention also relates to a procedure for their preparation and to pharmaceutical compositions containing them. These compounds are antihypertensive and bronchodilator agents.
