新型氨基噻二唑酰胺作为选择性EP(3)受体拮抗剂的发现
Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.
作者信息
Hilfiker Mark A, Wang Ning, Hou Xiaoping, Du Zhimin, Pullen Mark A, Nord Melanie, Nagilla Rakesh, Fries Harvey E, Wu Charlene W, Sulpizio Anthony C, Jaworski Jon-Paul, Morrow Dwight, Edwards Richard M, Jin Jian
机构信息
Department of Medicinal Chemistry, Metabolic Pathways Center of Excellence for Drug Discovery, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, United States.
出版信息
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4292-5. doi: 10.1016/j.bmcl.2009.05.074. Epub 2009 May 27.
This Letter discloses a series of 2-aminothiadiazole amides as selective EP(3) receptor antagonists. SAR optimization resulted in compounds with excellent functional activity in vitro. In addition, efforts to optimize DMPK properties in the rat are discussed. These efforts have resulted in the identification of potent, selective EP(3) receptor antagonists with excellent DMPK properties suitable for in vivo studies.
本信函披露了一系列作为选择性EP(3)受体拮抗剂的2-氨基噻二唑酰胺。构效关系优化产生了在体外具有优异功能活性的化合物。此外，还讨论了在大鼠中优化药物代谢动力学性质的努力。这些努力已导致鉴定出具有优异药物代谢动力学性质、适用于体内研究的强效、选择性EP(3)受体拮抗剂。
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