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Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity |
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| Authors: | Kevin K-C Liu Bruce A Lefker Mark A Dombroski Phoebe Chiang Peter Cornelius Terrell A Patterson Yuan Zeng Stephanie Santucci Elizabeth Tomlinson Colleen P Gibbons Ravi Marala Janice A Brown Jimmy X Kong Eunsun Lee Wendy Werner Zane Wenzel Craig Giragossian Hou Chen Steven B Coffey |
| Institution: | 1. Pfizer Global Research and Development, Chemistry Department, 10770 Science Center Drive, La Jolla, CA 92120, United States;2. Pfizer Global Research and Development, Groton Laboratories, 558 Eastern Point Road, Groton, CT 06340, United States |
| Abstract: | Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered. |
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