2. Academic Validation
  3. Novel and potent small-molecule urotensin II receptor agonists

Novel and potent small-molecule urotensin II receptor agonists

  • Bioorg Med Chem. 2009 Jul 1;17(13):4657-65. doi: 10.1016/j.bmc.2009.04.062.
Fredrik Lehmann 1,  Erika A Currier,  Bryan Clemons,  Lars K Hansen,  Roger Olsson,  Uli Hacksell,  Kristina Luthman
Affiliations

Affiliation

  • 1 Department of Chemistry, Medicinal Chemistry, University of Gothenburg, Göteborg, Sweden.
PMID: 19481466 DOI: 10.1016/j.bmc.2009.04.062
Abstract

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).

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-10661
    UTII receptor Agonist