1138451-95-2Relevant academic research and scientific papers
Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity
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
scheme or table, p. 266 - 271 (2010/04/24)
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-clinical food intake model.
