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

Novel potent and efficacious nonpeptidic urotensin II receptor agonists.

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  • 1Department of Chemistry, Medicinal Chemistry, and Department of Chemistry, Organic Chemistry, Göteborg University, SE-412 96 Göteborg, Sweden, Acadia Pharmaceuticals AB, Medeon Science Park, SE-205 12 Malmö, Sweden.

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).

PMID:
16570919
[PubMed - indexed for MEDLINE]
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