Title of article :
Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis Original Research Article
Author/Authors :
Jing Su، نويسنده , , Brian A. McKittrick، نويسنده , , Haiqun Tang، نويسنده , , Michael Czarniecki، نويسنده , , William J. Greenlee، نويسنده , , Brian E. Hawes، نويسنده , , Kim O’Neill، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
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.
Keywords :
Antagonist , Melanin-concentrating hormone receptor R1 (MCH R1) , Obesity , High-throughput synthesis
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry
