Discovery of novel aminothiadiazole amides as selective EP 3 receptor antagonists

…, Z Du, MA Pullen, M Nord, R Nagilla, HE Fries…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4292 - 4295

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被引用次数: 24

摘要

This Letter discloses a series of 2-aminothiadiazole amides as selective EP3 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 EP3 receptor antagonists with excellent DMPK properties suitable for in vivo studies.