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Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Zhu, Yuping; de Jesus, Reynalda K; Tang, Haifeng; Walsh, Shawn P; Jiang, Jinlong; Gu, Xin; Teumelsan, Nardos; Shahripour, Aurash; Pio, Barbara; Ding, Fa-Xiang; Ha, Sookhee; Priest, Birgit T; Swensen, Andrew M; Alonso-Galicia, Magdalena; Felix, John P; Brochu, Richard M; Bailey, Timothy; Thomas-Fowlkes, Brande; Zhou, Xiaoyan; Pai, Lee-Yuh; Hampton, Caryn; Hernandez, Melba; Owens, Karen; Ehrhart, Juliann; Roy, Sophie; Kaczorowski, Gregory J; Yang, Lihu; Parmee, Emma R; Sullivan, Kathleen; Garcia, Maria L; Pasternak, Alexander.
Afiliação
  • Zhu Y; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States. Electronic address: yuping_zhu@merck.com.
  • de Jesus RK; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Tang H; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Walsh SP; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Jiang J; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Gu X; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Teumelsan N; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Shahripour A; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Pio B; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Ding FX; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Ha S; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Priest BT; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Swensen AM; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Alonso-Galicia M; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Felix JP; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Brochu RM; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Bailey T; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Thomas-Fowlkes B; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Zhou X; Department of Cardiometabolic Diseases, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Pai LY; Department of Cardiometabolic Diseases, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Hampton C; Department of Cardiometabolic Diseases, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Hernandez M; Department of Cardiometabolic Diseases, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Owens K; Pharmacokinetics, Pharmacodynamics and Drug Metabolism, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Ehrhart J; Department of Safety Assessment & Laboratory Animal Resources, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Roy S; Department of Cardiometabolic Diseases, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Kaczorowski GJ; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Yang L; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Parmee ER; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Sullivan K; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Garcia ML; Department of Pharmacology, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
  • Pasternak A; Discovery Chemistry, Merck Research Laboratories, Kenilworth, NJ 07033, United States.
Bioorg Med Chem Lett ; 26(23): 5695-5702, 2016 12 01.
Article em En | MEDLINE | ID: mdl-27839686
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oxazinas / Canais de Potássio Corretores do Fluxo de Internalização Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oxazinas / Canais de Potássio Corretores do Fluxo de Internalização Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2016 Tipo de documento: Article