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Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.
Joshi, Pramod; Anderson, Corey; Binch, Hayley; Hadida, Sabine; Yoo, Sanghee; Bergeron, Danielle; Decker, Caroline; terHaar, Ernst; Moore, Jonathan; Garcia-Guzman, Miguel; Termin, Andreas.
Afiliación
  • Joshi P; Vertex Pharmaceuticals Inc., Department of Chemistry and Drug Innovation, 11010 Torreyana Road, San Diego, CA 92121, United States.
  • Anderson C; Vertex Pharmaceuticals Inc., Department of Chemistry and Drug Innovation, 11010 Torreyana Road, San Diego, CA 92121, United States.
  • Binch H; Vertex Pharmaceuticals Inc., Department of Chemistry and Drug Innovation, 11010 Torreyana Road, San Diego, CA 92121, United States.
  • Hadida S; Vertex Pharmaceuticals Inc., Department of Chemistry and Drug Innovation, 11010 Torreyana Road, San Diego, CA 92121, United States.
  • Yoo S; Vertex Pharmaceuticals Inc., Department of Biology, 11010 Torreyana Road, San Diego, CA 92121, United States.
  • Bergeron D; Vertex Pharmaceuticals Inc., Department of Biology, 11010 Torreyana Road, San Diego, CA 92121, United States.
  • Decker C; Vertex Pharmaceuticals Inc., Department of Drug Metabolism and Pharmacokinetics, 11010 Torreyana Road, San Diego, CA 92121, United States.
  • terHaar E; Vertex Pharmaceuticals Inc., Department of Structural Biology, 130 Waverly Street, Cambridge, MA 02139, United States.
  • Moore J; Vertex Pharmaceuticals Inc., Department of Structural Biology, 130 Waverly Street, Cambridge, MA 02139, United States.
  • Garcia-Guzman M; Aspyrian Therapeutics Inc., 11189 Sorrento Valley Rd, San Diego CA 92121, United States. Electronic address: Miguel_Guzman@aspyriantherapeutics.com.
  • Termin A; Vertex Pharmaceuticals Inc., Department of Chemistry and Drug Innovation, 11010 Torreyana Road, San Diego, CA 92121, United States. Electronic address: andreas_termin@vrtx.com.
Bioorg Med Chem Lett ; 24(3): 845-9, 2014 Feb 01.
Article en En | MEDLINE | ID: mdl-24405707
ABSTRACT
Calcitonin gene-related peptide (CGRP) has been implicated in acute migraine pathogenesis. In an effort to identify novel CGRP receptor antagonists for the treatment of migraine, we have discovered thiazolidinone 49, a potent (Ki=30 pM, IC50=1 nM), orally bioavailable, CNS-penetrant CGRP antagonist with good pharmacokinetic properties.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Urea / Receptores de Péptido Relacionado con el Gen de Calcitonina / Tiazolidinedionas / Dipéptidos / Quinazolinonas Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Urea / Receptores de Péptido Relacionado con el Gen de Calcitonina / Tiazolidinedionas / Dipéptidos / Quinazolinonas Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article País de afiliación: Estados Unidos