title: Fragment-based discovery and optimization of BACE1 inhibitors.
abstract: A novel series of 2-aminobenzimidazole inhibitors of BACE1 has been discovered using fragment-based drug discovery (FBDD) techniques. The rapid optimization of these inhibitors using structure-guided medicinal chemistry is discussed.
authors.affiliation: Evotec UK Ltd, Abingdon, UK. james.madden@evotec.com
authors.forename: James
authors.initials: J
authors.lastname: Madden
authors.forename: Jenny R
authors.initials: JR
authors.lastname: Dod
authors.forename: Robert
authors.initials: R
authors.lastname: Godemann
authors.forename: Joachim
authors.initials: J
authors.lastname: Kraemer
authors.forename: Myron
authors.initials: M
authors.lastname: Smith
authors.forename: Marion
authors.initials: M
authors.lastname: Biniszkiewicz
authors.forename: David J
authors.initials: DJ
authors.lastname: Hallett
authors.forename: John
authors.initials: J
authors.lastname: Barker
authors.forename: Jane D
authors.initials: JD
authors.lastname: Dyekjaer
authors.forename: Thomas
authors.initials: T
authors.lastname: Hesterkamp
mesh_terms: D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D006801:Humans; D008958:Models, Molecular; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D011480:Protease Inhibitors; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human