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Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.
Gong, Hua; Yang, Michael; Xiao, Zili; Doweyko, Arthur M; Cunningham, Mark; Wang, Jinhong; Habte, Sium; Holloway, Deborah; Burke, Christine; Shuster, David; Gao, Ling; Carman, Julie; Somerville, John E; Nadler, Steven G; Salter-Cid, Luisa; Barrish, Joel C; Weinstein, David S.
Afiliación
  • Gong H; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Yang M; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Xiao Z; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Doweyko AM; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Cunningham M; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Wang J; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Habte S; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Holloway D; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Burke C; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Shuster D; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Gao L; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Carman J; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Somerville JE; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Nadler SG; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Salter-Cid L; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Barrish JC; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States.
  • Weinstein DS; Department of Discovery Chemistry, Immunoscience, Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, United States. Electronic address: David.Weinstein@bms.com.
Bioorg Med Chem Lett ; 24(15): 3268-73, 2014 Aug 01.
Article en En | MEDLINE | ID: mdl-24980053
ABSTRACT
Acylureas and acyclic imides are found to be excellent isosteres for 2-acylamino-1,3,4-thiadiazole in the azaxanthene-based series of glucocorticoid receptor (GR) agonists. The results reported herein show that primary acylureas maintain high affinity and selectivity for GR while providing improved CYP450 inhibition and pharmacokinetic profile over 2-acylamino-1,3,4-thiadiazoles. General methods for synthesis of a variety of acylureas and acyclic imides from a carboxylic acid were utilized and are described.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Tiadiazoles / Urea / Receptores de Glucocorticoides / Descubrimiento de Drogas / Compuestos Heterocíclicos con 3 Anillos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article País de afiliación: Estados Unidos
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Tiadiazoles / Urea / Receptores de Glucocorticoides / Descubrimiento de Drogas / Compuestos Heterocíclicos con 3 Anillos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article País de afiliación: Estados Unidos