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Discovery of ONO-8590580: A novel, potent and selective GABAA α5 negative allosteric modulator for the treatment of cognitive disorders.
Lewis, A; Beresford, A; Chambers, M S; Clark, G; Hartley, D C; Hirst, K L; Higashino, M; Kawahadara, S; Nakanishi, M; Saito, T; Imagawa, A; Habashita, H; Maidment, S; Macleod, A M; Owens, A P; Rae, A; Rouse, C; Wishart, G.
Afiliación
  • Lewis A; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Beresford A; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Chambers MS; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Clark G; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Hartley DC; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Hirst KL; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Higashino M; Ono Pharmaceutical Co. Ltd., Minase Research Institute, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.
  • Kawahadara S; Ono Pharmaceutical Co. Ltd., Minase Research Institute, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.
  • Nakanishi M; Ono Pharmaceutical Co. Ltd., Minase Research Institute, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.
  • Saito T; Ono Pharmaceutical Co. Ltd., Minase Research Institute, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.
  • Imagawa A; Ono Pharmaceutical Co. Ltd., Minase Research Institute, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.
  • Habashita H; Ono Pharmaceutical Co. Ltd., Minase Research Institute, Shimamoto-cho, Mishima-gun, Osaka 618-8585, Japan.
  • Maidment S; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Macleod AM; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Owens AP; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Rae A; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom. Electronic address: alastair.rae@crl.com.
  • Rouse C; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
  • Wishart G; Charles River Discovery Research Services, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, United Kingdom.
Bioorg Med Chem Lett ; 30(22): 127536, 2020 11 15.
Article en En | MEDLINE | ID: mdl-32898695
The identification and SAR development of a series of negative allosteric modulators of the GABAA α5 receptor is described. This novel series of compounds was optimised to provide analogues with high GABAA α5 binding affinity, high α5 negative allosteric modulatory activity, good functional subtype selectivity and low microsomal turnover, culminating in identification of ONO-8590580.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Trastornos del Conocimiento / Receptores de GABA-A / Descubrimiento de Drogas / Imidazoles Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Reino Unido Pais de publicación: Reino Unido
Texto completo
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Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piridinas / Trastornos del Conocimiento / Receptores de GABA-A / Descubrimiento de Drogas / Imidazoles Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Reino Unido Pais de publicación: Reino Unido