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Piperazinyl-oxadiazoles as selective sphingosine-1-phosphate receptor agonists.
Horan, Joshua C; Sanyal, Sulagna; Choi, Younggi; Hill-Drzewi, Melissa; Patnaude, Lori; Anderson, Shawn; Fogal, Steve; Mao, Can; Cook, Brian N; Gueneva-Boucheva, Kristina; Fisher, Michael B; Hickey, Eugene; Pack, Edward; Bannen, Lynne C; Chan, Diva S; Mac, Morrison B; Ng, Stephanie M; Wang, Yong; Xu, Wei; Modis, Louise K; Lemieux, René M.
Afiliação
  • Horan JC; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States. Electronic address: josh.horan@boehringer-ingelheim.com.
  • Sanyal S; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Choi Y; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Hill-Drzewi M; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Patnaude L; Inflammation and Immunology, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Anderson S; Inflammation and Immunology, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Fogal S; Inflammation and Immunology, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Mao C; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Cook BN; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Gueneva-Boucheva K; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Fisher MB; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Hickey E; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Pack E; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Bannen LC; Medicinal Chemistry, Exelixis, 210 East Grand Avenue, South San Francisco, CA 94080, United States.
  • Chan DS; Medicinal Chemistry, Exelixis, 210 East Grand Avenue, South San Francisco, CA 94080, United States.
  • Mac MB; Medicinal Chemistry, Exelixis, 210 East Grand Avenue, South San Francisco, CA 94080, United States.
  • Ng SM; Medicinal Chemistry, Exelixis, 210 East Grand Avenue, South San Francisco, CA 94080, United States.
  • Wang Y; Medicinal Chemistry, Exelixis, 210 East Grand Avenue, South San Francisco, CA 94080, United States.
  • Xu W; Medicinal Chemistry, Exelixis, 210 East Grand Avenue, South San Francisco, CA 94080, United States.
  • Modis LK; Inflammation and Immunology, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
  • Lemieux RM; Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, 900 Ridgebury Rd, Ridgefield, CT 06877, United States.
Bioorg Med Chem Lett ; 24(20): 4807-11, 2014 Oct 15.
Article em En | MEDLINE | ID: mdl-25241927
ABSTRACT
The discovery of a new series of selective S1P1 agonists is described. This series of piperazinyl-oxadiazole derivatives was rapidly optimized starting from high-throughput screening hit 1 to afford potent and selective lead compound 10d. Further SAR studies showed that 10d was converted to the active phosphate metabolite 29 in vivo. Oral administration of compound 10d to rats was shown to induce lymphopenia at 3 mg/kg.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Oxidiazóis / Piperazinas / Receptores de Lisoesfingolipídeo Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Oxidiazóis / Piperazinas / Receptores de Lisoesfingolipídeo Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2014 Tipo de documento: Article