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Discovery of substituted biphenyl imidazoles as potent,bioavailable bombesin receptor subtype-3 agonists |
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| Authors: | Shuwen He Peter H. Dobbelaar Jian Liu Tianying Jian Iyassu K. Sebhat Linus S. Lin Allan Goodman Cheng Guo Peter R. Guzzo Mark Hadden Alan J. Henderson Megan Ruenz Bruce J. Sargent Larry Yet Theresa M. Kelly Oksana Palyha Yanqing Kan Jie Pan Howard Chen Donald J. Marsh Ravi P. Nargund |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA;2. Albany Molecular Research Institute, 26 Corporate Circle, Albany, NY 12203, USA;3. Department of Obesity Research, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA;4. Department of Pharmacology, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA |
| Abstract: | We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3. |
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