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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 |
| 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: | 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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