151978-58-4Relevant articles and documents
Azerocyclic compounds and their uses
-
, (2022/01/20)
The present invention proposes a nitrogen heterocyclic compound and its use, in particular, the present invention proposes a new compound that effectively inhibits ATX, which is a compound shown in the formula below, or a tautomer of the compound shown be
Tandem Gold-Catalyzed Dehydrative Cyclization/Diels-Alder Reactions: Facile Access to Indolocarbazole Alkaloids
Borrero, Nicholas V.,Deratt, Lindsey G.,Ferreira Barbosa, Lais,Abboud, Khalil A.,Aponick, Aaron
, p. 1754 - 1757 (2015/04/14)
A gold-catalyzed synthesis of cyclic 2-oxodienes from readily prepared propargyl alcohols and the subsequent Diels-Alder reaction are reported. The dehydrative cyclization reactions proceeded smoothly, and the dienes formed in situ were demonstrated to un
Synthesis of a potent photoreactive acidic γ-secretase modulator for target identification in cells
Rennhack, Andreas,Bulic, Bruno,Jumpertz, Thorsten,Ness, Julia,Baches, Sandra,Weggen, Sascha,Pietrzik, Claus U.
supporting information, p. 6523 - 6532,10 (2012/12/12)
Supramolecular self-assembly of amyloidogenic peptides is closely associated with numerous pathological conditions. For instance, Alzheimers disease (AD) is characterized by abundant amyloid plaques originating from the proteolytic cleavage of the amyloid precursor protein (APP) by β- and γ-secretases. Compounds named γ-secretase modulators (GSMs) can shift the substrate cleavage specificity of γ-secretase toward the production of non-amyloidogenic, shorter Aβ fragments. Herein, we describe the synthesis of highly potent acidic GSMs, equipped with a photoreactive diazirine moiety for photoaffinity labeling. The probes labeled the N-terminal fragment of presenilin (the catalytic subunit of γ-secretase), supporting a mode of action involving binding to γ-secretase. This fundamental step toward the elucidation of the molecular mechanism governing the GSM-induced shift in γ-secretase proteolytic specificity should pave the way for the development of improved drugs against AD.
