An example of designed multiple ligands spanning protein classes: Dual MCH-1R antagonists/DPPIV inhibitors

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• 作者：William T. Gattrell^a ; ^{wgattrell@yahoo.co.uk} ; Colin P. Sambrook Smith^a ; Alun J. Smith^b
• 关键词：Designed multiple ligands ; Type II diabetes ; MCH-1R ; DPPIV
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 April, 2012
• 卷：22
• 期：7
• 页码：2464-2469
• 文件大小：436 K

摘要

A ligand-based approach to identify potential starting points for a dual MCH-1R antagonist/DPPIV inhibitor medicinal chemistry program was undertaken. Potential ligand pairs were identified by analysis of MCH-1R and DPPIV in vitro data. A highly targeted synthetic effort lead to the discovery of pyridone 11, a dual MCH-1R antagonist/DPPIV inhibitor with selectivity over DPP8 and DPP9.