发现嘧啶甲酰胺类化合物作为强效和选择性 CCK1 受体激动剂。
Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.
机构信息
Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):2911-5. doi: 10.1016/j.bmcl.2011.03.069. Epub 2011 Mar 31.
PMID:21493064
Abstract
A series of six-membered heterocycle carboxamides were synthesized and evaluated as cholecystokinin 1 receptor (CCK1R) agonists. A pyrimidine core proved to be the best heterocycle, and SAR studies resulted in the discovery of analog 5, a potent and structurally diverse CCK1R agonist.
摘要
合成了一系列六元杂环酰胺，并对其作为胆囊收缩素 1 受体（CCK1R）激动剂进行了评估。嘧啶核被证明是最好的杂环，SAR 研究发现了类似物 5，一种具有高活性和结构多样性的 CCK1R 激动剂。
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