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Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
Truong, Anh P; Aubele, Danielle L; Probst, Gary D; Neitzel, Martin L; Semko, Chris M; Bowers, Simeon; Dressen, Darren; Hom, Roy K; Konradi, Andrei W; Sham, Hing L; Garofalo, Albert W; Keim, Pamela S; Wu, Jing; Dappen, Michael S; Wong, Karina; Goldbach, Erich; Quinn, Kevin P; Sauer, John-Michael; Brigham, Elizabeth F; Wallace, William; Nguyen, Lan; Hemphill, Susanna S; Bova, Michael P; Bard, Frédérique; Yednock, Ted A; Basi, Guriqbal.
Affiliation
  • Truong AP; Department of Medicinal Chemistry, Elan Pharmaceuticals, 800 Gateway Boulevard, South San Francisco, CA 94080, USA.
Bioorg Med Chem Lett ; 19(17): 4920-3, 2009 Sep 01.
Article in En | MEDLINE | ID: mdl-19660943
In this Letter, we report our strategy to design potent and metabolically stable gamma-secretase inhibitors that are efficacious in reducing the cortical Abetax-40 levels in FVB mice via a single PO dose.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protease Inhibitors / Pyrazoles / Quinolines / Sulfonamides / Amyloid Precursor Protein Secretases Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Type: Article Affiliation country: United States
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Protease Inhibitors / Pyrazoles / Quinolines / Sulfonamides / Amyloid Precursor Protein Secretases Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Type: Article Affiliation country: United States