Peptidotriazolamers Inhibit A beta(1-42) Oligomerization and Cross a Blood-Brain-Barrier Model

Tonali, Nicolo
Hericks, Loreen
Schroeder, David C.
Kracker, Oliver
Krzemieniecki, Radoslaw
Kaffy, Julia
Le Joncour, Vadim
Laakkonen, Pirjo
Marıon, Antoıne
Ongeri, Sandrine
Dodero, Veronica I.
Sewald, Norbert
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 beta (A beta) 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" (KLVFF20)-L-16 and G(39)VVIA(42) in A beta(1-42). We found that peptidotriazolamers act as modulators of the A beta(1-42) oligomerization. Some peptidotriazolamers are able to interfere with the formation of toxic early A beta 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.


Palladium-catalyzed formation of oxazolidinones from biscarbamates: a mechanistic study
Kilbas, Benan; Balci, Metin (Beilstein Institut, 2011-2-24)
Oxazolidinones can be synthesized starting from cyclic biscarbamates via a palladium-catalyzed reaction. To test the proposed mechanism of this reaction, first, bicyclonorcarene endoperoxides derived from cyano and carbomethoxy cycloheptatrienes were synthesized and converted into the corresponding diols. The reaction of diols with toluenesulfonyl isocyanate followed by a palladium catalyzed reaction furnished oxazolidinone derivatives in similar yields. It was shown that, if one face of the double bond is ...
Polystyrene-b-poly(2-vinyl phenacyl pyridinium) salts as photoinitiators for free radical and cationic polymerizations and their photoinduced molecular associations
Taskin, Omer Suat; Erel Göktepe, İrem; Khan, Muhammad Alyaan Ahmed; Pispas, Stergios; Yağcı, Yusuf (Elsevier BV, 2014-07-01)
Polystyrene-b-poly(2-vinyl phenacyl pyridinium hexafluorophosphate) (PS-b-PVPP) was synthesized by reacting polystyrene-b-poly(2-vinyl pyridine) prepared by living anionic polymerization with phenacyl bromide followed by counter anion exchange reaction. The ability of PS-b-PVPP to act as a photoinitiator for both free radical and cationic polymerizations is demonstrated. In the free radical polymerization, the initiation step involves the decay of the excited state of the salt with homolytic bond rupture of...
Aminophosphine-palladium(II) complexes: Synthsesis, structure and applications in Suzuki and Heck cross-coupling reactions
AYDEMİR, MURAT; BAYSAL, AKIN; ŞAHİN, Ertan; Gumgum, Bahattin; Özkar, Saim (Elsevier BV, 2011-11-30)
Reaction of furfurylamine with 1 or 2 equivalents of PPh2Cl in the presence of Et3N, proceeds under anaerobic conditions in thf to give furfuryl-2-(N-diphenylphosphino)amine, Ph2PNHCH2-C4H3O, 1 and furfuryl-2-(N,N-bis(diphenylphosphino)amine), (Ph2P)(2)NCH2-C4H3O, 2, respectively. The reactions of 1 and 2 with MCl2(cod) (M = Pd, Pt; cod = 1,5-cyclooctadiene) or Pt(CH3)(2)(cod) yield complexes [M(Ph2PNHCH2-C4H3O)(2)Cl-2] (M= Pd 1a, Pt 1b), [Pt(Ph2PNHCH2-C4H3O)(2)(CH3)(2)] (1c), and [M((Ph2P)(2) NCH2-C4H3O)Cl...
lntrazeolite Metal Carbonyl Kinetics: 12CO Substitution in Mo(12C0)6-Na56Y by PMe3 and 13CO
OZIN, GA; Özkar, Saim; PASTORE, HO; POE, AJ; VICHI, EJS (Royal Society of Chemistry (RSC), 1991-02-01)
The first kinetic study is reported for archetypical substitution reactions of PMe3 and 13CO with the well defined intrazeolite system, Mo(12CO)6-Na56Y, for which excellent isosbestic points and first order behaviour are obtained, the activation parameters indicate a highly ordered 'supramolecular' transition state consisting of activated Mo(12CO)6 and PMe3 or 13CO all anchored to the Na+ ions in the alpha-cage of the host lattice.
Synthesis and characterization of epoxy-acrylate vinylester resin and network structure
Zeytin Derin, Çiğdem; Usanmaz, Ali; Department of Polymer Science and Technology (2008)
Vinylesters are termosets resins that have reactive double bond at the chain ends. They are produced by the reaction of various epoxies and acrylic acids by step growth polymerization. Vinylester chains are oligomers with molecular weight from 600 to 1200 g/mol. The resin viscosity is very high; therefore, diluent is used for easy application. The generally used diluent is styrene with, reactive double bonds to form a crosslink between the chains. The diluted resin viscosities are between 200 2000 cps. Per...
Citation Formats
N. Tonali et al., “Peptidotriazolamers Inhibit A beta(1-42) Oligomerization and Cross a Blood-Brain-Barrier Model,” CHEMPLUSCHEM, pp. 0–0, 2021, Accessed: 00, 2021. [Online]. Available: