title: Triazoles as γ-secretase modulators.
abstract: Synthesis, SAR, and evaluation of aryl triazoles as novel gamma secretase modulators (GSMs) are presented in this communication. Starting from the literature and in-house leads, we evaluated a range of five-membered heterocycles as replacements for olefins commonly found in non-acid GSMs. 1,2,3-C-aryl-triazoles were identified as suitable replacements which exhibited good modulation of γ-secretase activity, excellent pharmacokinetics and good central lowering of Aβ42 in Sprague-Dawley rats.
authors: Merck Research Laboratories Boston, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. christian_fischer@merck.com
authors: Christian
authors: C
authors: Fischer
authors: Susan L
authors: SL
authors: Zultanski
authors: Hua
authors: H
authors: Zhou
authors: Joey L
authors: JL
authors: Methot
authors: W Colby
authors: WC
authors: Brown
authors: Dawn M
authors: DM
authors: Mampreian
authors: Adam J
authors: AJ
authors: Schell
authors: Sanjiv
authors: S
authors: Shah
authors: Hugh
authors: H
authors: Nuthall
authors: Bethany L
authors: BL
authors: Hughes
authors: Nadja
authors: N
authors: Smotrov
authors: Candia M
authors: CM
authors: Kenific
authors: Jonathan C
authors: JC
authors: Cruz
authors: Deborah
authors: D
authors: Walker
authors: Melanie
authors: M
authors: Bouthillette
authors: George N
authors: GN
authors: Nikov
authors: Dan F
authors: DF
authors: Savage
authors: Valentina V
authors: VV
authors: Jeliazkova-Mecheva
authors: Damaris
authors: D
authors: Diaz
authors: Alexander A
authors: AA
authors: Szewczak
authors: Nathan
authors: N
authors: Bays
authors: Richard E
authors: RE
authors: Middleton
authors: Benito
authors: B
authors: Munoz
authors: Mark S
authors: MS
authors: Shearman