title: Design of potent inhibitors of human beta-secretase. Part 1.
abstract: We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.
authors.affiliation: Pfizer Inc., 700N. Chesterfield Pkwy., St. Louis, MO 63198, USA. john.n.freskos@pfizer.com
authors.forename: John N
authors.initials: JN
authors.lastname: Freskos
authors.forename: Yvette M
authors.initials: YM
authors.lastname: Fobian
authors.forename: Timothy E
authors.initials: TE
authors.lastname: Benson
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Bienkowski
authors.forename: David L
authors.initials: DL
authors.lastname: Brown
authors.forename: Thomas L
authors.initials: TL
authors.lastname: Emmons
authors.forename: Robert
authors.initials: R
authors.lastname: Heintz
authors.forename: Alice
authors.initials: A
authors.lastname: Laborde
authors.forename: Joseph J
authors.initials: JJ
authors.lastname: McDonald
authors.forename: Brent V
authors.initials: BV
authors.lastname: Mischke
authors.forename: John M
authors.initials: JM
authors.lastname: Molyneaux
authors.forename: Joseph B
authors.initials: JB
authors.lastname: Moon
authors.forename: Patrick B
authors.initials: PB
authors.lastname: Mullins
authors.forename: D
authors.initials: D
authors.lastname: Bryan Prince
authors.forename: Donna J
authors.initials: DJ
authors.lastname: Paddock
authors.forename: Alfredo G
authors.initials: AG
authors.lastname: Tomasselli
authors.forename: Gregory
authors.initials: G
authors.lastname: Winterrowd
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy*; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D011487:Protein Conformation; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry*; D013450:Sulfones / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D011480:Protease Inhibitors; D013449:Sulfonamides; D013450:Sulfones; D053829:Amyloid Precursor Protein Secretases