6096-81-7Relevant articles and documents
Gold nanoparticle-based probe for colorimetric detection of copper ions
Chai, Weiwei,Feng, Qingyue,Nie, Meijuan,Wang, Chong,Jiang, Yangjing,Zheng, Huimin,Li, Mei-Jin
, p. 502 - 506 (2017)
A new ligand 10-mercaptodecyl-1-iminodiacetic acid (MDIA) was synthesized and used to modify gold nanoparticles to provide a simple assay to repeatedly sense Cu2+ in the solution at room temperature. This functionalized gold nanosensor was applied for the detection of Cu2+ in water samples with sensitivity and simplicity. The chelation/aggregation process is reversible via addition of a strong metal ion chelator such as EDTA. This simple and fast colorimetric sensor is important in the application of copper ion detection in water quality during the emergency and early warning monitoring.
Synthesis of Deuterated or Tritiated Glycine and Its Methyl Ester
Shevchenko,Andreeva,Nagaev, I. Yu.,Myasoedov
, p. 266 - 267 (2019/01/03)
Abstract: Heating glycine (Gly) and methyl glycinate (GlyOCH3) supported on 5% Pd/C or 5% Pt/C in a deuterium or tritium gas atmosphere gave the isotope-labeled products. The experiments were carried out at 180°C for 10 min. The deuterium atom inclusion under these conditions averaged up to 1.8 atoms per molecule for Gly and up to 1.0 atom per molecule for GlyOCH3. The reaction with tritium gas gave labeled products with a specific radioactivity of 27–31 Ci/mmol for Gly and 18 Ci/mmol for GlyOCH3.
Structure-activity relationships of imidazole-derived 2-[ N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme
Charton, Julie,Gauriot, Marion,Totobenazara, Jane,Hennuyer, Nathalie,Dumont, Julie,Bosc, Damien,Marechal, Xavier,Elbakali, Jamal,Herledan, Adrien,Wen, Xiaoan,Ronco, Cyril,Gras-Masse, Helene,Heninot, Antoine,Pottiez, Virginie,Landry, Valerie,Staels, Bart,Liang, Wenguang G.,Leroux, Florence,Tang, Wei-Jen,Deprez, Benoit,Deprez-Poulain, Rebecca
, p. 547 - 567 (2015/03/18)
Insulin degrading enzyme (IDE) is a zinc metalloprotease that degrades small amyloid peptides such as amyloid-a and insulin. So far the dearth of IDE-specific pharmacological inhibitors impacts the understanding of its role in the physiopathology of Alzheimer's disease, amyloid-a clearance, and its validation as a potential therapeutic target. Hit 1 was previously discovered by high-throughput screening. Here we describe the structure-activity study, that required the synthesis of 48 analogues. We found that while the carboxylic acid, the imidazole and the tertiary amine were critical for activity, the methyl ester was successfully optimized to an amide or a 1,2,4-oxadiazole. Along with improving their activity, compounds were optimized for solubility, lipophilicity and stability in plasma and microsomes. The docking or co-crystallization of some compounds at the exosite or the catalytic site of IDE provided the structural basis for IDE inhibition. The pharmacokinetic properties of best compounds 44 and 46 were measured in vivo. As a result, 44 (BDM43079) and its methyl ester precursor 48 (BDM43124) are useful chemical probes for the exploration of IDE's role.