Document Report Card

ID: ALA1146083

Journal: J Med Chem

Title: Novel potent and efficacious nonpeptidic urotensin II receptor agonists.

Authors: Lehmann F, Pettersen A, Currier EA, Sherbukhin V, Olsson R, Hacksell U, Luthman K.

Abstract: 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 (pEC(50) 7.49).

CiteXplore: 16570919

DOI: 10.1021/jm051121i