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Design,synthesis and SAR of substituted indoles as selective TrkA inhibitors
Authors:Danielle M. Hurzy  Darrell A. Henze  Tamara D. Cabalu  Kartik Narayan  Amanda Heller  Andrew J. Cooke
Affiliation:1. Department of Medicinal Chemistry, MRL, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA;2. Department of Pain Research, MRL, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA;3. Department of Drug Metabolism, MRL, Merck & Co., Inc., 770 Sumneytown Pike, West Point, PA 19486, USA;4. Analytical Process and Technology, Sanofi Pasteur, Discovery Drive, Swiftwater, PA 18370, USA;5. Scientific Operations, Lab Connect, LLC., 605 First Avenue, Ste. 300, Seattle, WA 98104, USA
Abstract:A series of substituted indoles were examined as selective inhibitors of tropomyosin-related kinase receptor A (TrkA), a therapeutic target for the treatment of pain. An SAR optimization campaign based on ALIS screening lead compound 1 is reported.
Keywords:TrkA  Pain  Indoles
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