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

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.

Afiliação

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 em En | MEDLINE | ID: mdl-19487124

ABSTRACT

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.

Assuntos

Amidas/química; Química Farmacêutica/métodos; Receptores de Prostaglandina E/antagonistas & inibidores; Receptores de Prostaglandina E/química; Tiadiazóis/química; Administração Oral; Animais; Cães; Desenho de Fármacos; Humanos; Modelos Químicos; Estrutura Molecular; Ligação Proteica; Ratos; Ratos Sprague-Dawley; Receptores de Prostaglandina E Subtipo EP3; Relação Estrutura-Atividade

Texto completo

Imprimir

XML

PubMed Links

Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Tiadiazóis / Química Farmacêutica / Receptores de Prostaglandina E / Amidas Idioma: En Ano de publicação: 2009 Tipo de documento: Article

Texto completo

Imprimir

XML

PubMed Links

Buscar no Google