Optimization of isochromanone based urotensin II receptor agonists

…, JN Ma, ES Burstein, U Hacksell, K Luthman

Index: Lehmann, Fredrik; Currier, Erika A.; Olsson, Roger; Ma, Jian-Nong; Burstein, Ethan S.; Hacksell, Uli; Luthman, Kristina Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 13 p. 4844 - 4854

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Citation Number: 7

Abstract

A series of novel isochromanone based urotensin II receptor agonists have been synthesized and evaluated for their activity using a functional cell based assay (R-SAT). Several potent and efficacious derivatives were identified with 3-(3, 4-dichlorophenyl)-6, 7- dimethyl-3-(2-dimethylaminoethyl) isochroman-1-one (28) being the most potent compound showing an EC50-value of 51nM, thereby being the most potent compound so far within ...