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Thiazole-diamides as potent gamma-secretase inhibitors.
Chen, Yuhpyng L; Cherry, Kevin; Corman, Michael L; Ebbinghaus, Charles F; Gamlath, Chandra B; Liston, Dane; Martin, Barbara-Anne; Oborski, Christine E; Sahagan, Barbara G.
Afiliação
  • Chen YL; Department of Medicinal Chemistry, PGRD, Pfizer Inc., Connecticut, Groton, CT 06340, USA. yuhpyng888@yahoo.com
Bioorg Med Chem Lett ; 17(20): 5518-22, 2007 Oct 15.
Article em En | MEDLINE | ID: mdl-17764937
ABSTRACT
The thiazole-diamide series (1) has been identified as highly potent gamma-secretase inhibitors. Several representative compounds showed IC(50) values of <0.3 nM. The synthesis and SAR, as well as a radiolabeled synthesis of [(3)H]-2a, are described.
Assuntos
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Base de dados: MEDLINE Assunto principal: Tiazóis / Diamida / Secretases da Proteína Precursora do Amiloide Idioma: En Ano de publicação: 2007 Tipo de documento: Article
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Base de dados: MEDLINE Assunto principal: Tiazóis / Diamida / Secretases da Proteína Precursora do Amiloide Idioma: En Ano de publicação: 2007 Tipo de documento: Article