Novel and potent small-molecule urotensin II receptor agonists
A series of analogs of the non-peptidic urotensin II receptor agonist N-[1-(4-chlorophenyl)-3-(dimethylamino)propyl]-4-phenylbenzamide (FL104) has been synthesized and evaluated pharmacologically. The enantiomers of the two most potent racemic analogues were obtained from the corresponding diastereomeric mandelic amides. In agreement with previously observed SAR, most of the agonist potency resided in the (S) enantiomers. The most potent UII receptor agonist in the new series was (S)-N-[3-dimethylamino-1-(2-naphthyl)propyl]-4-(4-chlorophenyl)benzamide (EC50 = 23 nM at the urotensin II receptor).
Lehmann, Fredrik,Currier, Erika A.,Clemons, Bryan,Hansen, Lars K.,Olsson, Roger,Hacksell, Uli,Luthman, Kristina
experimental part
p. 4657 - 4665
(2009/12/06)
UII-MODULATING COMPOUNDS AND THEIR USE
Disclosed herein are novel aromatic-containing compounds and methods for using various aromatic-containing compounds for treatment and prevention of diseases and disorders related to the Urotensin II receptor.
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Page/Page column 75-76
(2008/12/05)
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