261912-63-4

Upstream product

• 87156-40-9 1-amino-2-azidoethane 
• 98-59-9 p-toluenesulfonyl chloride 
• 3634-89-7 N-(p-toluenesulfonyl)aziridine 
• 6367-75-5 2-(tosylamino)ethyl p-toluenesulfonate 
• 4556-90-5 N-(2-bromo-ethyl)-4-methyl-benzenesulfonamide 
• 6331-00-6 N-(2-chloroethyl)-4-methylbenzenesulfonamide 
• 19263-22-0 1-azido-2-bromoethane 

Downstream Products

• 14316-16-6 N-tosylethylenediamine 
• 1416133-69-1 1-[2-(p-toluenesulfonamido)ethyl]-1H-1,2,3-triazole-4,5-dicarboxylic acid 

Relevant academic research and scientific papers

An alternative modular 'click-SNAr-click' approach to develop subcellular localised fluorescent probes to image mobile Zn2+

Zn2+ is involved in a number of biological processes and its wide-ranging roles at the subcellular level, especially in specific organelles, have not yet been fully established due to a lack of tools to image it effectively. We report a new and

Forthrightly monitoring ferroptosis induced by endoplasmic reticulum stresses through fluorescence lifetime imaging of microviscosity increases with a specific rotor

To test the hypothesis that the microviscosity changes of Endoplasmic Reticulum (ER) can be a useful indicator of ferroptosis promoted by ER Stresses (ERS), a new ER targeting viscosity rotor, L-Vis-1 was developed and applied in the quantitation of visco

An efficient and controlled synthesis of persulfonylated G1 dendrimers: Via click reaction

This work presents the first report, we believe, on controlled synthesis of clickable dendrimers using aromatic and heteroaromatic cores and persulfonylated dendrons. Owing to poor thermal stability of persulfonylated dendrons, CuAAC reaction conditions w

The development of a versatile trifunctional scaffold for biological applications

We describe the synthesis of a trifunctional scaffold constructed from a planar core of trimesic acid derivatized with three propargylamine moieties. The scaffold was attached to a solid-phase resin through the carboxylic group of a fluorinated alkyl spacer arm. The orthogonal protection of two of the alkyne groups with triethylsilyl and triisopropylsilyl moieties enabled modular and efficient derivatization of the scaffold with three different azides by using solid-phase synthesis on amphiphilic ChemMatrix resin. We showed that a fluorine label can be used to quantify the content of fluorine-containing compounds by 19F NMR spectroscopic analysis after cleavage from the resin. We have thus designed a versatile and convenient tool that could be useful for simple and rapid solid-phase syntheses of combinatorial libraries of the scaffold-based compounds, for example as new protein binders. The development of a trifunctional scaffold derivatized with three orthogonally protected alkyne moieties that is useful for the solid-phase synthesis of combinatorial libraries is described.

Fragment-based discovery of novel and selective mPGES-1 inhibitors Part 1: Identification of sulfonamido-1,2,3-triazole-4,5-dicarboxylic acid

Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible prostaglandin E synthase that catalyzes the conversion of prostaglandin PGH 2 to PGE2 and represents a novel target for therapeutic treatment of inflammatory disorders. It is essential to identify mPGES-1 inhibitor with novel scaffold as new hit or lead compound for the purpose of the next-generation anti-inflammatory drugs. Herein we report the discovery of sulfonamido-1,2,3-triazole-4,5-dicarboxylic derivatives as a novel class of mPGES-1 inhibitors identified through fragment-based virtual screening and in vitro assays on the inhibitory activity of the actual compounds. 1-[2-(N-Phenylbenzenesulfonamido)ethyl]-1H-1,2,3-triazole-4,5-dicarboxylic acid (6f) inhibits human mPGES-1 (IC50 of 1.1 μM) with high selectivity (ca.1000-fold) over both COX-1 and COX-2 in a cell-free assay. In addition, the activity of compound 6f was again tested at 10 μM concentration in presence of 0.1% Triton X-100 and found to be reduced to 1/4 of its original activity without this detergent. Compared to the complete loss of activity of nuisance inhibitor with the detergent, therefore, compound 6f would be regarded as a partial nuisance inhibitor of mPGES-1 with a novel scaffold for the optimal design of more potent mPGES-1 inhibitors.

Effective ring-opening reaction of aziridines with trimethylsilyl compounds: A facile access to β-amino acids and 1,2-diamine derivatives

Ring-opening reactions of aziridines with trimethylsilyl compounds triggered by tetrabutylammonium fluoride give the corresponding products regioselectively in excellent yield. It provides a facile and efficient procedure for the ring-opening reactions of