Novel and potent small-molecule urotensin II receptor agonists
Research output: Contribution to journal › Article
A series of analogs of the non-peptidic urotensin II receptor agonist N-[1-(4-chlorophenyl)-3-(dimethylamino)propyl]-4-phenylbenzamide (FL104) has been synthesized and evaluated pharmacologically. The enantiomers of the two most potent racemic analogues were obtained from the corresponding diastereomeric mandelic amides. In agreement with previously observed SAR, most of the agonist potency resided in the (S) enantiomers. The most potent UII receptor agonist in the new series was (S)-N-[3-dimethylamino-1-(2-naphthyl)propyl]-4-(4-chlorophenyl)benzamide (EC 50 = 23 nM at the urotensin II receptor).
|Research areas and keywords||
Subject classification (UKÄ) – MANDATORY
|Journal||Bioorganic and Medicinal Chemistry|
|Publication status||Published - 2009 Jul 1|