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ID: ALA1153033

Journal: Bioorg Med Chem Lett

Title: Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.

Authors: Hilfiker MA, Wang N, Hou X, Du Z, Pullen MA, Nord M, Nagilla R, Fries HE, Wu CW, Sulpizio AC, Jaworski JP, Morrow D, Edwards RM, Jin J.

Abstract: 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.

CiteXplore: 19487124

DOI: 10.1016/j.bmcl.2009.05.074