885672-75-3

Upstream product

• 885672-69-5 1-(4-chlorophenyl)-N³,N³-dimethylpropane-1,3-diamine 
• 933-88-0 ortho-toluoyl chloride 
• 118-90-1 ortho-methylbenzoic acid 
• 2138-38-7 1-(4-chlorophenyl)-3-dimethylamino-1-propanone 
• 16254-21-0 3-(dimethylamino)-1-(4-chlorobenzene)-1-propanol 

Relevant academic research and scientific papers

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.

Novel potent and efficacious nonpeptidic urotensin II receptor agonists

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).