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