title: Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.
abstract: The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.
authors: Pfizer Global Research and Development, Pfizer Inc., St. Louis Laboratories, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA. steve.kortum@pfizer.com
authors: Steven W
authors: SW
authors: Kortum
authors: Timothy E
authors: TE
authors: Benson
authors: Michael J
authors: MJ
authors: Bienkowski
authors: Thomas L
authors: TL
authors: Emmons
authors: D Bryan
authors: DB
authors: Prince
authors: Donna J
authors: DJ
authors: Paddock
authors: Alfredo G
authors: AG
authors: Tomasselli
authors: Joseph B
authors: JB
authors: Moon
authors: Alice
authors: A
authors: LaBorde
authors: Ruth E
authors: RE
authors: TenBrink
mesh_terms: D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D000818:Animals; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D002402:Cathepsin D / Q000037:antagonists & inhibitors; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D005021:Ethylamines / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D006860:Hydrogen Bonding; D007069:Ifosfamide / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D051379:Mice; D018345:Mice, Knockout; D008956:Models, Chemical; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D005021:Ethylamines; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human; C509282:Bace1 protein, mouse; D002402:Cathepsin D; D007069:Ifosfamide