60343-28-4

Upstream product

• 2067-33-6 5-bromopentanoic acid 
• 100-51-6 benzyl alcohol 
• 1927-62-4 tetrahydro-2-(benzyloxy)-2H-pyran 
• 4509-90-4 5-bromovaleroyl chloride 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 709657-09-0 5-[3-(3,4-bis-benzyloxyphenyl)-2-(N'-tert-butoxycarbonylhydrazino)-2-methylpropionyl]oxypentanoic acid benzyl ester 
• 305835-89-6 benzyl 5-[(1,2-dihydro-1,2-dioxonaphth-4-yl)oxy]valerate 
• 957130-01-7 C₄₇H₅₈N₄O₈ 
• 1202041-15-3 benzyl 5-(2-nitrophenylthio)pentanoate 

Relevant academic research and scientific papers

Cationic Lipid

The present invention provides a cationic lipid which is able to be used for nucleic acid delivery to the cytoplasm. A cationic lipid according to the present invention is, for example, a compound represented by formula (1) or a pharmaceutically acceptable salt thereof, wherein L1 and L2 independently represent an alkylene group having 3 to 10 carbon atoms; R1 and R2 independently represent an alkyl group having 4 to 24 carbon atoms or an alkenyl group having 4 to 24 carbon atoms; R3 represents an alkyl group having 1 to 3 carbon atoms; and X1 represents a single bond or CO—O—.

Synthesis and evaluation of phenoxymethylbenzamide analogues as anti-trypanosomal agents

The synthesis and anti-trypanosomal activity of a compound library based on a phenoxymethylbenzamide hit discovered in a high throughput screen is described. Several of the analogues exhibited potent activity against Trypanosoma brucei rhodesiense, a human infective strain of the trypanosome parasite, that serve as lead compounds for further optimisation. This journal is

Multifunctional supramolecular dendrimers with an s-triazine ring as the central core: Liquid crystalline, fluorescence and photoconductive properties

Novel liquid crystal (LC) dendrimers have been synthesised by hydrogen bonding between an s-triazine as the central core and three peripheral dendrons derived from bis(hydroxymethyl)propionic acid. Symmetric acid dendrons bearing achiral promesogenic units have been synthesised to obtain 3:1 complexes with triazine that exhibit LC properties. Asymmetric dendrons that combine the achiral promesogenic unit and an active moiety derived from coumarin or pyrene structures have been synthesised in order to obtain dendrimers with photophysical and electrochemical properties. The formation of the complexes was confirmed by IR and NMR spectroscopy data. The liquid crystalline properties were investigated by differential scanning calorimetry, polarising optical microscopy and X-ray diffractometry. All complexes displayed mesogenic properties, which were smectic in the case of symmetric dendrons and their complexes and nematic in the case of asymmetric dendrons and their dendrimers. A supramolecular model for the lamellar mesophase, based mainly on X-ray diffraction studies, is proposed. The electrochemical behaviour of dendritic complexes was investigated by cyclic voltammetry. The UV/Vis absorption and emission properties of the compounds and the photoconductive properties of the dendrons and dendrimers were also investigated.

Supramolecular architectures from bent-core dendritic molecules

Control of the self-assembly of small molecules to generate architectures with diverse shapes and dimensions is a challenging research field. We report unprecedented results on the ability of ionic, bent dendritic molecules to aggregate in water. A range of analytical techniques (TEM, SEM, SAED, and XRD) provide evidence of the formation of rods, spheres, fibers, helical ribbons, or tubules from achiral molecules. The compact packing of the bent-core structures, which promotes the bent-core mesophases, also occurs in the presence of a poor solvent to provide products ranging from single objects to supramolecular gels. The subtle balance of molecule/solvent interactions and appropriate molecular designs also allows the transfer of molecular conformational chirality to morphological chirality in the overall superstructure. Functional motifs and controlled morphologies can be combined, thereby opening up new prospects for the generation of nanostructured materials through a bottom-up strategy.

MRI CONTRAST AGENTS

The present invention relates to MRI based imaging. In particular, the present invention provides MRI contrast agents targeted to a HaloTag protein with tunable relaxation properties thereby providing optimal relaxivity for low field strength imaging and the other optimal relaxivity for high field strength imaging. Moreover, the MRI contrast agents are used to detect gene expression (of a gene of interest) in real time in vivo, to detect changes in gene expression (of a gene of interest) over time in, for example, an individual organism, to detect gene expression changes (of a gene of interest) in response to therapeutics, in cell labeling for MR imaging, in clinical diagnostics, and in theranostics.

7-DEAZAPURINE MODULATORS OF HISTONE METHYLTRANSFERASE, AND METHODS OF USE THEREOF

Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransf erases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.

Reporter protein-targeted probes for magnetic resonance imaging

Contrast agents for magnetic resonance imaging are frequently employed as experimental and clinical probes. Drawbacks include low signal sensitivity, fast clearance, and nonspecificity that limit efficacy in experimental imaging. In order to create a bioresponsive MR contrast agent, a series of four Gd(III) complexes targeted to the HaloTag reporter were designed and synthesized. HaloTag is unique among reporter proteins for its specificity, versatility, and the covalent interaction between substrate and protein. In similar systems, these properties produce prolonged in vivo lifetimes and extended imaging opportunities for contrast agents, longer rotational correlation times, and increases in relaxivity (r1) upon binding to the HaloTag protein. In this work we report a new MR contrast probe, 2CHTGd, which forms a covalent bond with its target protein and results in a dramatic increase in sensitivity. A 6-fold increase in r1, from 3.8 to 22 mM-1s-1, is observed upon 2CHTGd binding to the target protein. This probe was designed for use with the HaloTag protein system which allows for a variety of substrates (specific for MRI, florescence, or protein purification applications) to be used with the same reporter.

COMPOSITIONS AND METHODS FOR MAGNETIC RESONANCE IMAGING CONTRAST AGENTS

The present application provides for compositions and methods of creating and applying contrast agents that find use in magnetic resonance imaging (MRI). In particular, contrast agents that comprise monodisperse, protein polymer backbones capable of chelating multiple paramagnetic ions resulting in high relaxivity for use in enhancing MRI signal intensity.

Synthesis of benzyl diisopropyl 5-phosphonopentanoate and 5-phosphonopentanoic acid: An analog of succinyl phosphate

Benzyl 5-(diisopropoxyphosphoryl)pentanoate (benzyl diisopropyl 5-phosphonopentanoate) was synthesized from 5-bromopentanoic acid in three steps. The first step esterified 5-bromopentanoic acid with benzyl alcohol, the second step was a Finkelstein halogen exchange with sodium iodide, and the third step was a Michaelis-Arbuzov reaction. This compound was characterized by NMR and high-resolution mass spectrometry. This compound was hydrolyzed to produce 5-phosphonopentanoic acid, which is an analog of succinyl phosphate and a possible enzyme inhibitor. Copyright Taylor & Francis Group, LLC.