885672-64-0Relevant academic research and scientific papers
Novel potent and efficacious nonpeptidic urotensin II receptor agonists
Lehmann, Fredrik,Pettersen, Anna,Currier, Erika A.,Sherbukhin, Vladimir,Olsson, Roger,Hacksell, Uli,Luthman, Kristina
, p. 2232 - 2240 (2007/10/03)
Six different series of nonpeptidic urotensin II receptor agonists have been synthesized and evaluated for their agonistic activity in a cell-based assay (R-SAT). The compounds are ring-opened analogues of the isochromanone-based agonist AC-7954 with different functionalities constituting the linker between the two aromatic ring moieties. Several of the compounds are highly potent and efficacious, with N-[1-(4-chlorophenyl)-3-(dimethylamino)- propyl]-4-phenylbenzamide oxalate (5d) being the most potent. The pure enantiomers of 5d were obtained from the corresponding diastereomeric amides. It was shown by a combination of X-ray crystallography and chemical correlation that the activity resides in the S-enantiomer of 5d (pEC50 7.49).
UII-MODULATING COMPOUNDS AND THEIR USE
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Page/Page column 40, (2010/11/25)
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.
