Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis |
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| Authors: | Su Jing McKittrick Brian A Tang Haiqun Czarniecki Michael Greenlee William J Hawes Brian E O'Neill Kim |
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| Affiliation: | Department of Chemical Research, Schering-Plough Research Institute K15 2545, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jing.su@spcorp.com |
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| Abstract: | 
A structure-activity study on benzylpiperidine 1 was accomplished by utilizing high-throughput synthesis. Three focused libraries were designed and synthesized to quickly develop SAR. Further optimization led to the discovery of compound 2, an MCH receptor R1 antagonist with over 400-fold improvement in biological activity over the original lead. |
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