593247-65-5

Upstream product

• 100-39-0 benzyl bromide 
• 267876-32-4 ethyl 3-hydroxy-6-methyl-2-oxo-1,2-dihydropyridine-4-carboxylate 
• 40876-98-0 sodium 1,4-diethoxy-1,4-dioxobut-2-en-2-olate 
• 88330-76-1 diethyl oxalacetate sodium salt 
• 267875-78-5 3-benzyloxy-6-methyl-2-oxo-1,2-dihydropyridine-4-carboxylic acid ethyl ester 

Downstream Products

• 593247-66-6 3-benzyloxy-6-methyl-4-(2-thioxothiazolidine-3-carbonyl)-1[H]-pyridin-2-one 
• 953392-74-0 3-benzyloxy-4-(2-ethanolcarbamoyl)-6-methyl-2(1H)-pyridinone 
• 593247-67-7 N,N,N,-tris[3-benzyloxy-6-methyl-2(1H)-pyridinone-4-carboxylamideethyl]amine 

Relevant academic research and scientific papers

Structure-Activity Relationships in Metal-Binding Pharmacophores for Influenza Endonuclease

Metalloenzymes represent an important target space for drug discovery. A limitation to the early development of metalloenzyme inhibitors has been the lack of established structure-activity relationships (SARs) for molecules that bind the metal ion cofactor(s) of a metalloenzyme. Herein, we employed a bioinorganic perspective to develop an SAR for inhibition of the metalloenzyme influenza RNA polymerase PAN endonuclease. The identified trends highlight the importance of the electronics of the metal-binding pharmacophore (MBP), in addition to MBP sterics, for achieving improved inhibition and selectivity. By optimization of the MBPs for PAN endonuclease, a class of highly active and selective fragments was developed that displays IC50 values 50 values of ～10 nM, illustrating the utility of a metal-centric development campaign in generating highly active and selective metalloenzyme inhibitors.

A double-3, 2 - hydroxy pyridine ketone derivative and its preparation and use (by machine translation)

The invention discloses a double-3, 2 - hydroxy pyridine ketone derivative and its preparation and use, is characterized in that the double 3, 2 - hydroxy pyridine ketone derivatives in order to monochloride, succinic acid alkone sodium salt derivative an

2-HYDROXY-1-OXO 1,2 DIHYDRO ISOQUINOLINE CHELATING AGENTS

The invention provides a new class of strongly chelating multidentate ligands based on a 2-hydroxy-1-oxo-1,2-dihydro-isoquinoline-3-carboxylic acid scaffold (hereafter 1,2-HOIQO) in combination with polyamine backbones. The extremely stable bidentate 1,2- HOIQO moiety can be synthesized by standard synthetic methodology on a large scale. An advantageous feature is the possibility to introduce a wide range of substituents on the benzene ring by standard transformations (like electrophilic aromatic substitutions). This allows, for example, for the tuning of chemical, photophysical, and solubility properties, as well as the attachment of functional moieties, relevant for sensing and imaging applications (e.g. DNA, proteins, antibodies, fluorophores, etc.). The combination of the 1,2-HOIQO chelators with polyamine backbones provides very strongly binding ligands for a variety of metals including first-row transition metals, lanthanides, actinides, etc. Metal complexes of this kind are expected to be useful in a number of applications (e.g. luminescence, MRI, actinide sequestering, metal chelation therapy, metal radioisotope labeling, etc.).

Hydroxypyridonate and hydroxypyrimidinone chelating agents

The present invention provides hydroxypyridinone and hydroxypyrimidone chelating agents. Also provides are Gd(III) complexes of these agents, which are useful as contrast enhancing agents for magnetic resonance imaging. The invention also provides methods of preparing the compounds of the invention, as well as methods of using the compounds in magnetic resonance imaging applications.