title: Quinazolinones as γ-secretase modulators.
abstract: Synthesis, SAR and evaluation of styrenyl quinazolinones as novel gamma secretase modulators are presented in this communication. Starting from literature and in-house leads we evaluated a range of quinazolinones which showed good modulation of γ-secretase activity.
authors.affiliation: Merck Research Laboratories Boston, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. christian_fischer@merck.com
authors.forename: Christian
authors.initials: C
authors.lastname: Fischer
authors.forename: Sanjiv
authors.initials: S
authors.lastname: Shah
authors.forename: Bethany L
authors.initials: BL
authors.lastname: Hughes
authors.forename: George N
authors.initials: GN
authors.lastname: Nikov
authors.forename: Jamie L
authors.initials: JL
authors.lastname: Crispino
authors.forename: Richard E
authors.initials: RE
authors.lastname: Middleton
authors.forename: Alexander A
authors.initials: AA
authors.lastname: Szewczak
authors.forename: Benito
authors.initials: B
authors.lastname: Munoz
authors.forename: Mark S
authors.initials: MS
authors.lastname: Shearman
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy / Q000201:enzymology / Q000378:metabolism; D053829:Amyloid Precursor Protein Secretases / Q000378:metabolism*; D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D002460:Cell Line; D006801:Humans; D020128:Inhibitory Concentration 50; D010446:Peptide Fragments / Q000037:antagonists & inhibitors / Q000378:metabolism; D011485:Protein Binding; D052999:Quinazolinones / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D016229:Amyloid beta-Peptides; D010446:Peptide Fragments; D052999:Quinazolinones; C078592:amyloid beta-protein (1-40); C075222:amyloid beta-protein (1-42); D053829:Amyloid Precursor Protein Secretases