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Discovery and optimization of oxadiazole-based FLAP inhibitors.
Bartolozzi, Alessandra; Abeywardane, Asitha; Bosanac, Todd; Broadwater, John A; Chen, Zhidong; Hutzler, J Matthew; Huber, John D; Nemoto, Peter; Olague, Alan; Riether, Doris; Simpson, Tom; Takahashi, Hidenori; Wu, Lifen; Zhang, Yunlong; Zindell, Renee M.
Afiliação
  • Bartolozzi A; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA. Electronic address: abartolozzi@gmail.com.
  • Abeywardane A; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Bosanac T; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Broadwater JA; CardioMetabolic Diseases Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Chen Z; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Hutzler JM; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Huber JD; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Nemoto P; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Olague A; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Riether D; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Simpson T; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Takahashi H; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Wu L; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Zhang Y; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
  • Zindell RM; Small Molecule Discovery Research, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, CT 06877-0368, USA.
Bioorg Med Chem Lett ; 27(20): 4652-4659, 2017 10 15.
Article em En | MEDLINE | ID: mdl-28927794
Structure activity relationship (SAR) investigation of an oxadiazole based series led to the discovery of several potent FLAP inhibitors. Lead optimization focused on achieving functional activity while improving physiochemical properties and reducing hERG inhibition. Several compounds with favorable in vitro and in vivo properties were identified that were suitable for advanced profiling.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Oxidiazóis / Proteínas Ativadoras de 5-Lipoxigenase / Inibidores da Proteína Ativadora de 5-Lipoxigenase Limite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Oxidiazóis / Proteínas Ativadoras de 5-Lipoxigenase / Inibidores da Proteína Ativadora de 5-Lipoxigenase Limite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article