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Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity |
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| Authors: | Souers Andrew J Gao Ju Wodka Dariusz Judd Andrew S Mulhern Mathew M Napier James J Brune Michael E Bush Eugene N Brodjian Sevan J Dayton Brian D Shapiro Robin Hernandez Lisa E Marsh Kennan C Sham Hing L Collins Christine A Kym Philip R |
| Affiliation: | Metabolic Disease Research, Abbott Laboratories, Abbott Park, IL 60064, USA. andrew.souers@abbott.com |
| Abstract: |  A series of urea-based N-1-(2-aminoethyl)-indazoles was synthesized and evaluated for melanin-concentrating hormone receptor 1 (MCHr1) antagonism in both binding and functional assays. Several compounds that acted as MCHr1 antagonists were identified, and optimization afforded a compound with excellent binding affinity, good functional potency, and oral efficacy in a chronic model for weight loss in diet-induced obese mice. |
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