title: Anilinotriazoles as potent gamma secretase modulators.
abstract: The design and synthesis of a novel series of potent gamma secretase modulators is described. Exploration of various spacer groups between the triazole ring and the aromatic appendix in 2 has led to anilinotriazole 28, which combined high in vitro and in vivo potency with an acceptable drug-like profile.
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium. Electronic address: ivelter@its.jnj.com.
authors.forename: Adriana I
authors.initials: AI
authors.lastname: Velter
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: François P
authors.initials: FP
authors.lastname: Bischoff
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Didier
authors.initials: D
authors.lastname: Berthelot
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Michel
authors.initials: M
authors.lastname: De Cleyn
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Daniel
authors.initials: D
authors.lastname: Oehlrich
authors.affiliation: Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Libuse
authors.initials: L
authors.lastname: Jaroskova
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Gregor
authors.initials: G
authors.lastname: Macdonald
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Garrett
authors.initials: G
authors.lastname: Minne
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Serge
authors.initials: S
authors.lastname: Pieters
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Frederik
authors.initials: F
authors.lastname: Rombouts
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Sven
authors.initials: S
authors.lastname: Van Brandt
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Yves
authors.initials: Y
authors.lastname: Van Roosbroeck
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Michel
authors.initials: M
authors.lastname: Surkyn
authors.affiliation: Neuroscience, Janssen Research & Development, Jarama 75, 45007 Toledo, Spain.
authors.forename: Andrés A
authors.initials: AA
authors.lastname: Trabanco
authors.affiliation: Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Gary
authors.initials: G
authors.lastname: Tresadern
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Tongfei
authors.initials: T
authors.lastname: Wu
authors.affiliation: Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Herman
authors.initials: H
authors.lastname: Borghys
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Marc
authors.initials: M
authors.lastname: Mercken
authors.affiliation: Discovery Sciences, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
authors.forename: Chantal
authors.initials: C
authors.lastname: Masungi
authors.affiliation: Neuroscience, Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium. Electronic address: hgijsen@its.jnj.com.
authors.forename: Harrie
authors.initials: H
authors.lastname: Gijsen
mesh_terms: D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000737:chemistry / Q000378:metabolism; D000814:Aniline Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D001921:Brain / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D051379:Mice; D008822:Mice, Transgenic; D011485:Protein Binding; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism
chemical_list: D016229:Amyloid beta-Peptides; D000814:Aniline Compounds; D014230:Triazoles; D053829:Amyloid Precursor Protein Secretases; C023650:aniline
keywords: Alzheimer’s disease; Anilinotriazoles; Gamma secretase modulators