Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity

…, TA Patterson, Y Zeng, S Santucci, E Tomlinson…

Index: Liu, Kevin K.-C.; Cornelius, Peter; Patterson, Terrell A.; Zeng, Yuan; Santucci, Stephanie; Tomlinson, Elizabeth; Gibbons, Colleen; Maurer, Tristan S.; Marala, Ravi; Brown, Janice; Kong, Jimmy X.; Lee, Eunsun; Werner, Wendy; Wenzel, Zane; Vage, Chandra Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 1 p. 266 - 271

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Citation Number: 12

Abstract

Based on our original pyrazine hit, CP-0809101, novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Synthesis and structure–activity relationship (SAR) studies are described with emphasis on optimization of the selectivity against 5HT2a and 5HT2b receptors with excellent 2c potency. Orally-active and selective compounds were identified with dose–responsive in vivo efficacy in our pre- ...