100841-19-8Relevant articles and documents
Peptidotriazolamers Inhibit Aβ(1–42) Oligomerization and Cross a Blood-Brain-Barrier Model
Tonali, Nicolo,Hericks, Loreen,Schr?der, David C.,Kracker, Oliver,Krzemieniecki, Rados?aw,Kaffy, Julia,Le Joncour, Vadim,Laakkonen, Pirjo,Marion, Antoine,Ongeri, Sandrine,Dodero, Veronica I.,Sewald, Norbert
, p. 840 - 851 (2021)
In peptidotriazolamers every second peptide bond is replaced by a 1H-1,2,3-triazole. Such foldamers are expected to bridge the gap in molecular weight between small-molecule drugs and protein-based drugs. Amyloid β (Aβ) aggregates play an important role in Alzheimer's disease. We studied the impact of amide bond replacements by 1,4-disubstituted 1H-1,2,3-triazoles on the inhibitory activity of the aggregation “hot spots” K16LVFF20 and G39VVIA42 in Aβ(1–42). We found that peptidotriazolamers act as modulators of the Aβ(1–42) oligomerization. Some peptidotriazolamers are able to interfere with the formation of toxic early Aβ oligomers, depending on the position of the triazoles, which is also supported by computational studies. Preliminary in vitro results demonstrate that a highly active peptidotriazolamer is also able to cross the blood-brain-barrier.
N-[4-phenyl-3-(benzoylamino)-1,1,1-trifluoro-butyl-2-yl]-phenylalaninol derivative as well as preparation method and application thereof
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Paragraph 0051-0056, (2020/11/23)
The present invention discloses an N-[4-phenyl-3-(benzoylamino)-1,1,1-trifluoro-butyl-2-yl]-phenylalaninol derivative, which is a compound represented by a general formula I and a pharmaceutically acceptable salt or hydrate thereof, and wherein R1 and R3
Enantioconservative synthesis and ring closing metathesis of disubstituted dialkenic amides
Sauriat-Dorizon, Helene,Guibe, Francois
, p. 6711 - 6714 (2007/10/03)
Optically pure disubstituted dialkenic amides 2, which are direct precursors of Z-ethylenic pseudo-peptides 1, are readily synthesized and then cyclized to lactams 3 in the presence of Grubbs' ruthenium-based metathesis catalysts with total conservation of enantiomeric purity.