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Pyridazine-derived γ-secretase modulators.
Wan, Zehong; Hall, Adrian; Jin, Yun; Xiang, Jia-Ning; Yang, Eric; Eatherton, Andrew; Smith, Beverley; Yang, Guang; Yu, Haihua; Wang, Ju; Ye, Liang; Lau, Lit-Fui; Yang, Ting; Mitchell, William; Cai, Wei; Zhang, Xiaomin; Sang, Yingxia; Wang, Yonghui; Tong, Zhaolong; Cheng, Ziqiang; Hussain, Ishrut; Elliott, John D; Matsuoka, Yasuji.
Afiliación
  • Wan Z; Research and Development, GlaxoSmithKline Pharmaceuticals, 898 Halei Road, Zhangjiang Hi-tech Park, Pudong, Shanghai 201023, China. zehong.2.wan@gsk.com
Bioorg Med Chem Lett ; 21(13): 4016-9, 2011 Jul 01.
Article en En | MEDLINE | ID: mdl-21636276
ABSTRACT
SAR of a novel series of pyridazine-derived γ-secretase modulators is described. Compound 25 was found to be a potent modulator in vitro, which on further profiling, was found to decrease Aß42 and Aß40, and maintain the levels of total Aß. Furthermore, 25 demonstrated excellent pharmacokinetic parameters as well as good CNS penetration in the rat.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridazinas / Secretasas de la Proteína Precursora del Amiloide Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2011 Tipo del documento: Article País de afiliación: China
Texto completo
Imprimir
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PubMed Links
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Piridazinas / Secretasas de la Proteína Precursora del Amiloide Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2011 Tipo del documento: Article País de afiliación: China