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