Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis

…, H Tang, M Czarniecki, WJ Greenlee, BE Hawes…

Index: Su, Jing; McKittrick, Brian A.; Tang, Haiqun; Czarniecki, Michael; Greenlee, William J.; Hawes, Brian E.; O'Neill, Kim Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 5 p. 1829 - 1836

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Citation Number: 21

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.