Isochromanone-based urotensin-II receptor agonists.

  title={Isochromanone-based urotensin-II receptor agonists.},
  author={Fredrik Lehmann and Erika A Currier and Roger Olsson and Uli Hacksell and Kristina Luthman},
  journal={Bioorganic & medicinal chemistry},
  volume={13 8},
A series of analogues of the selective non-peptide urotensin II (UII) receptor agonist 3-(4-chlorophenyl)-3-(2-dimethylaminoethyl)-isochroman-1-one (AC-7954, 1) was synthesized and evaluated for UII agonist activity using a functional cell-based assay. The introduction of a methyl group in the 4-position resulted in a complete loss of activity, whereas substituents in the aromatic rings were beneficial. Sterically demanding amino groups were also detrimental to the activity. Several potent… CONTINUE READING