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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.
  • 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 en En | MEDLINE | ID: mdl-28927794
ABSTRACT
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 Banco de datos: MEDLINE Asunto principal: Oxadiazoles / Proteínas Activadoras de la 5-Lipooxigenasa / Inhibidores de Proteína Activante de 5-Lipoxigenasa Límite: Animals / Humans / Male Idioma: En Año: 2017 Tipo del documento: Article
Texto completo
Imprimir
XML
PubMed Links
Search on Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Oxadiazoles / Proteínas Activadoras de la 5-Lipooxigenasa / Inhibidores de Proteína Activante de 5-Lipoxigenasa Límite: Animals / Humans / Male Idioma: En Año: 2017 Tipo del documento: Article