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Novel Potent and Efficacious Nonpeptidic Urotensin II Receptor Agonists

Novel Potent and Efficacious Nonpeptidic Urotensin II Receptor Agonists

Fredrik Lehmann, Anna Pettersen, Erika A Currier, Vladimir Sherbukhin, Roger Olsson, Uli Hacksell, Kristina Luthman

J Med Chem. 2006 Apr 6;49(7):2232-40.

PMID: 16570919

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).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP477313090	AC-7954		477313-09-0	Price

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