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Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.
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.
Affiliation
  • Hilfiker MA; Department of Medicinal Chemistry, Metabolic Pathways Center of Excellence for Drug Discovery, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, United States. mark.a.hilfiker@gsk.com
Bioorg Med Chem Lett ; 19(15): 4292-5, 2009 Aug 01.
Article in En | MEDLINE | ID: mdl-19487124
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiadiazoles / Chemistry, Pharmaceutical / Receptors, Prostaglandin E / Amides Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Document type: Article Affiliation country: Estados Unidos
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Thiadiazoles / Chemistry, Pharmaceutical / Receptors, Prostaglandin E / Amides Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Document type: Article Affiliation country: Estados Unidos