title: Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
abstract: 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.
authors: Department of Medicinal Chemistry, Elan Pharmaceuticals, 800 Gateway Boulevard, South San Francisco, CA 94080, USA.
authors: Anh P
authors: AP
authors: Truong
authors: Danielle L
authors: DL
authors: Aubele
authors: Gary D
authors: GD
authors: Probst
authors: Martin L
authors: ML
authors: Neitzel
authors: Chris M
authors: CM
authors: Semko
authors: Simeon
authors: S
authors: Bowers
authors: Darren
authors: D
authors: Dressen
authors: Roy K
authors: RK
authors: Hom
authors: Andrei W
authors: AW
authors: Konradi
authors: Hing L
authors: HL
authors: Sham
authors: Albert W
authors: AW
authors: Garofalo
authors: Pamela S
authors: PS
authors: Keim
authors: Jing
authors: J
authors: Wu
authors: Michael S
authors: MS
authors: Dappen
authors: Karina
authors: K
authors: Wong
authors: Erich
authors: E
authors: Goldbach
authors: Kevin P
authors: KP
authors: Quinn
authors: John-Michael
authors: JM
authors: Sauer
authors: Elizabeth F
authors: EF
authors: Brigham
authors: William
authors: W
authors: Wallace
authors: Lan
authors: L
authors: Nguyen
authors: Susanna S
authors: SS
authors: Hemphill
authors: Michael P
authors: MP
authors: Bova
authors: Frédérique
authors: F
authors: Bard
authors: Ted A
authors: TA
authors: Yednock
authors: Guriqbal
authors: G
authors: Basi
mesh_terms: D000284:Administration, Oral; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D015195:Drug Design; D051379:Mice; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011720:Pyrazoles / Q000737:chemistry*; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry*
chemical_list: D011480:Protease Inhibitors; D011720:Pyrazoles; D011804:Quinolines; D013449:Sulfonamides; C031280:pyrazole; D053829:Amyloid Precursor Protein Secretases