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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 |
| Institution: | 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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