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Molecular hybridization yields triazole bronchodilators for the treatment of COPD.
Jones, Lyn H; Burrows, Jane; Feeder, Neil; Glossop, Paul; James, Kim; Jones, Rhys M; Kenyon, Amy S; Patel, Sheena; Roberts, Dannielle F; Selby, Matthew D; Strang, Ross S; Stuart, Emilio F; Trevethick, Michael A; Watson, Jessica; Wright, Karen N; Clarke, Nick.
Afiliación
  • Jones LH; WorldWide Medicinal Chemistry, 610 Main Street, Cambridge, MA 02139, USA. Electronic address: lyn.jones@pfizer.com.
  • Burrows J; Pharmaceutical Sciences, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Feeder N; Pharmaceutical Sciences, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Glossop P; WorldWide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • James K; WorldWide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Jones RM; Pharmacokinetics, Dynamics and Metabolism, 610 Main Street, Cambridge, MA 02139, USA.
  • Kenyon AS; WorldWide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Patel S; Allergy and Respiratory Biology, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK; CVMED Research Unit, Pfizer, Cambridge, MA 02139, USA.
  • Roberts DF; WorldWide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Selby MD; WorldWide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Strang RS; WorldWide Medicinal Chemistry, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Stuart EF; Allergy and Respiratory Biology, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Trevethick MA; Allergy and Respiratory Biology, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Watson J; Allergy and Respiratory Biology, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Wright KN; Allergy and Respiratory Biology, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK.
  • Clarke N; Allergy and Respiratory Biology, Pfizer, Ramsgate Road, Sandwich CT13 9NJ, UK; Inflammation and Immunology Research Unit, Pfizer, 610 Main Street, Cambridge, MA 02139, USA.
Bioorg Med Chem Lett ; 25(22): 5121-6, 2015 Nov 15.
Article en En | MEDLINE | ID: mdl-26471092
A 1,2,4-triazole motif was employed as a bioisostere for the ester commonly used in muscarinic antagonists, and subsequent integrative conjugation to a ß2 agonist quinolinone furnished a new class of bifunctional MABAs for the treatment of COPD. Medicinal chemistry optimization using the principles of 'inhalation by design' furnished a clinical candidate with desirable pharmacological, pharmacokinetic and biopharmaceutical properties.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Triazoles / Broncodilatadores / Antagonistas Muscarínicos / Enfermedad Pulmonar Obstructiva Crónica / Agonistas de Receptores Adrenérgicos beta 2 Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Triazoles / Broncodilatadores / Antagonistas Muscarínicos / Enfermedad Pulmonar Obstructiva Crónica / Agonistas de Receptores Adrenérgicos beta 2 Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2015 Tipo del documento: Article