Isochromanone-based urotensin-II receptor agonists

F Lehmann, EA Currier, R Olsson, U Hacksell…

Index: Lehmann, Fredrik; Currier, Erika A.; Olsson, Roger; Hacksell, Uli; Luthman, Kristina Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 8 p. 3057 - 3068

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Citation Number: 23

Abstract

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 ...