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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 |
| Affiliation: | 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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