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MgI2‐Mediated Chemoselective Cleavage of Protecting Groups: An Alternative to Conventional Deprotection Methodologies 下载免费PDF全文
Mathéo Berthet Florian Davanier Dr. Gilles Dujardin Prof. Jean Martinez Dr. Isabelle Parrot 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(31):11014-11016
The scope of MgI2 as a valuable tool for quantitative and mild chemoselective cleavage of protecting groups is described here. This novel synthetic approach expands the use of protecting groups, widens the concept of orthogonality in synthetic processes, and offers a facile opportunity to release compounds from solid supports. 相似文献
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Dr. Lech‐Gustav Milroy Dr. Maria Bartel Dr. Morkos A. Henen Dr. Seppe Leysen Joris M. C. Adriaans Prof. Dr. Luc Brunsveld Dr. Isabelle Landrieu Dr. Christian Ottmann 《Angewandte Chemie (International ed. in English)》2015,54(52):15720-15724
The discovery of novel protein–protein interaction (PPI) modulators represents one of the great molecular challenges of the modern era. PPIs can be modulated by either inhibitor or stabilizer compounds, which target different though proximal regions of the protein interface. In principle, protein–stabilizer complexes can guide the design of PPI inhibitors (and vice versa). In the present work, we combine X‐ray crystallographic data from both stabilizer and inhibitor co‐crystal complexes of the adapter protein 14‐3‐3 to characterize, down to the atomic scale, inhibitors of the 14‐3‐3/Tau PPI, a potential drug target to treat Alzheimer’s disease. The most potent compound notably inhibited the binding of phosphorylated full‐length Tau to 14‐3‐3 according to NMR spectroscopy studies. Our work sets a precedent for the rational design of PPI inhibitors guided by PPI stabilizer–protein complexes while potentially enabling access to new synthetically tractable stabilizers of 14‐3‐3 and other PPIs. 相似文献
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Barwick Vicki Ellison Stephen L. R. Gjengedal Elin Magnusson Bertil Molinier Olivier Patriarca Marina Sibbesen Lorens Vanlaethem Nicole Vercruysse Isabelle 《Accreditation and quality assurance》2017,22(5):253-263
Accreditation and Quality Assurance - Eurachem held a workshop on method validation in analytical sciences in Gent, Belgium, on 9–10 May 2016. A summary of the working group discussions is... 相似文献
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Bryan S. Holtzman Eric T. Roberts Nicholas S. Caminiti Jacob A. Fox Madison B. Goodstein Staci A. Hill Zitong B. Jia Isabelle N.-M. Leibler Michael L. Martini Gina M. Mendolia Sarah B. Nodder Molly S. Costanza-Robinson Richard C. Bunt 《Tetrahedron letters》2017,58(5):432-436
A nucleophile crossover experiment was used to monitor the reversibility of nucleophilic addition of benzylamine to π-allylpalladium complexes. Dppe, dppp, dppb, and PHOX showed more crossover than PPh3 and dppm in both DMF and dichloromethane. Crossover was inhibited by the addition of DBU or Cs2CO3, but much less elimination to diene side products was observed with Cs2CO3. Analysis of percent crossover vs. percent reaction completion using the PHOX ligand revealed that with added DBU or Cs2CO3 crossover only began occurring after 100% completion had been reached. 相似文献
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Seindé Touré Isabelle Dusfour Didier Stien Véronique Eparvier 《Tetrahedron letters》2017,58(38):3727-3729
Two new tetrahydrofuran derivatives, mucorinic acids A (1) and B (2) as well as the three known secondary metabolites dehydroabietic acid (3), Δ8-dihydroabietic acid (4) and 8-pimarenic acid (5) were isolated from a solid culture of the fungus Mucor spp. isolated on insect Acalymma bivittula. The structure of these compounds was elucidated by analysis of NMR and MS spectroscopic data. Compounds were tested in antimicrobial and insecticidal assays. Dehydroabietic acid exhibited moderate larvicidal activity on Aedes aegypti larvae with 65% mortality at 10 ppm. Both new compounds 1 and 2 showed interesting antibacterial activity on Staphylococcus aureus and methicillin resistant S. aureus with MIC values in the 8–16 μg/ml. 相似文献
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Sandy Theysgeur Benoit Cudennec Barbara Deracinois Claire Perrin Isabelle Guiller Anne Lepoudre Christophe Flahaut Rozenn Ravallec 《Molecules (Basel, Switzerland)》2021,26(1)
Like their owners, dogs and cats are more and more affected by overweight and obesity-related problems and interest in functional pet foods is growing sharply. Through numerous studies, fish protein hydrolysates have proved their worth to prevent and manage obesity-related comorbidities like diabetes. In this work, a human in vitro static simulated gastrointestinal digestion model was adapted to the dog which allowed us to demonstrate the promising effects of a tilapia byproduct hydrolysate on the regulation of food intake and glucose metabolism. Promising effects on intestinal hormones secretion and dipeptidyl peptidase IV (DPP-IV) inhibitory activity were evidenced. We identify new bioactive peptides able to stimulate cholecystokinin (CCK) and glucagon-like peptide 1 (GLP-1) secretions, and to inhibit the DPP-IV activity after a transport study through a Caco-2 cell monolayer. 相似文献