An example of designed multiple ligands spanning protein classes: Dual MCH-1R antagonists/DPPIV inhibitors
An example of designed multiple ligands spanning protein classes: Dual MCH-1R antagonists/DPPIV inhibitors
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DOI：
10.1016/j.bmcl.2012.02.010
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发表时间：
2012-04-01
影响因子：
2.7
通讯作者：
Smith, Alun J.
中科院分区：
文献类型：
--
作者：
Gattrell, William T.;Smith, Colin P. Sambrook;Smith, Alun J.
采用基于配体的方法确定MCH-1 R拮抗剂/DPPIV抑制剂双重药物化学项目的潜在起始点。通过分析MCH-1 R和DPPIV的体外数据鉴定潜在的配体对。高度靶向的合成努力导致吡啶酮11的发现，这是一种对DPP 8和DPP 9具有选择性的MCH-1 R拮抗剂/DPPIV双重抑制剂。(C)2012爱思唯尔有限公司版权所有。
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. (C) 2012 Elsevier Ltd. All rights reserved.