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The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.
Liddle, John; Beaufils, Benjamin; Binnie, Margaret; Bouillot, Anne; Denis, Alexis A; Hann, Michael M; Haslam, Carl P; Holmes, Duncan S; Hutchinson, Jon P; Kranz, Michael; McBride, Andrew; Mirguet, Olivier; Mole, Damian J; Mowat, Christopher G; Pal, Sandeep; Rowland, Paul; Trottet, Lionel; Uings, Iain J; Walker, Ann L; Webster, Scott P.
Afiliação
  • Liddle J; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. Electronic address: john.2.liddle@gsk.com.
  • Beaufils B; GlaxoSmithKline, Les Ulis, Paris, France.
  • Binnie M; Centre for Cardiovascular Science, University of Edinburgh, UK.
  • Bouillot A; GlaxoSmithKline, Les Ulis, Paris, France.
  • Denis AA; GlaxoSmithKline, Les Ulis, Paris, France.
  • Hann MM; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • Haslam CP; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • Holmes DS; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • Hutchinson JP; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • Kranz M; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • McBride A; Centre for Cardiovascular Science, University of Edinburgh, UK.
  • Mirguet O; GlaxoSmithKline, Les Ulis, Paris, France.
  • Mole DJ; MRC Centre for Inflammation Research, University of Edinburgh, UK.
  • Mowat CG; EastChem School of Chemistry, University of Edinburgh, UK.
  • Pal S; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • Rowland P; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • Trottet L; GlaxoSmithKline, Les Ulis, Paris, France.
  • Uings IJ; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • Walker AL; GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK.
  • Webster SP; Centre for Cardiovascular Science, University of Edinburgh, UK.
Bioorg Med Chem Lett ; 27(9): 2023-2028, 2017 05 01.
Article em En | MEDLINE | ID: mdl-28336141
ABSTRACT
A series of potent, competitive and highly selective kynurenine monooxygenase inhibitors have been discovered via a substrate-based approach for the treatment of acute pancreatitis. The lead compound demonstrated good cellular potency and clear pharmacodynamic activity in vivo.
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Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Pancreatite / Inibidores Enzimáticos / Quinurenina 3-Mono-Oxigenase Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Pancreatite / Inibidores Enzimáticos / Quinurenina 3-Mono-Oxigenase Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2017 Tipo de documento: Article