Category: 71255-09-9

Schroeder, Gretchen M. published the artcileDiscovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily, Application In Synthesis of 71255-09-9, the main research area is aminopyridinyloxy fluorophenyl dihydropyridine carboxamide preparation Met kinase inhibitor.

Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous solubility and kinase selectivity. Analog 10 demonstrated complete tumor stasis in a Met-dependent GTL-16 human gastric carcinoma xenograft model following oral administration. Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclin. safety profiles, 10 has been advanced into phase I clin. trials.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application In Synthesis of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Abebe, Felagot A. published the artcileDevelopment of a Rapid In Vitro Screening Assay Using Metabolic Inhibitors to Detect Highly Selective Anticancer Agents, Application of 2-Methoxynicotinaldehyde, the main research area is antitumor drug screening assay metabolic inhibitor.

Traditional long exposure (24-72 h) cell viability assays for identification of potential drug compounds can fail to identify compounds that are: (a) biol. active but not toxic and (b) inactive without the addition of a synergistic additive. Herein, we report the development of a rapid (1-2 h) compound screening technique using a com. available cell viability kit (CellTiter-Glo) that has led to the detection of compounds that were not identified as active agents using traditional cytotoxicity screening methods. These compounds, in combination with metabolic inhibitor 2-deoxyglucose, display selectivity toward a pancreatic cancer cell line. An evaluation of 11 mammalian cell lines against 30 novel compounds and two metabolic inhibitors is reported. The inclusion of metabolic inhibitors during an initial screening process, and not simply during mechanistic investigations of a previously identified hit compound, provides a rapid and sensitive tool for identifying drug candidates potentially overlooked by other methods.

ACS Omega published new progress about Antitumor agents. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application of 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wadsworth, Harry published the artcileExploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein-potential novel positron emitting tomography imaging agents, Formula: C7H7NO2, the main research area is PET imaging diaryl anilide preparation translocator protein ligand SAR.

A series of novel ligands based on the diaryl anilide (DAA) class of translocator protein (TSPO) ligands was synthesized and evaluated as potential positron emitting tomog. (PET) ligands for imaging TPSO in vivo. Fluorine-18 labeling of the mols. was achieved using direct radiolabelling or synthon based labeling approaches. Several of the ligands prepared have promising profiles as potential TSPO PET imaging ligands and will be evaluated further as potential clin. imaging agents.

Bioorganic & Medicinal Chemistry Letters published new progress about Brain. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Formula: C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kulathooran, S. published the artcileSynthesis and biological activities of novel heterocyclic chalcone derivatives by two different methods using anhydrous potassium carbonate as an efficient catalyst, SDS of cas: 71255-09-9, the main research area is acetyl dimethylfuran aryl aldehyde potassium carbonate catalyst microwave irradiation; chalcone preparation diastereoselective green chem antibacterial antifungal activity SAR.

A series of twenty 3-(aryl)-1-(2,5-dimethylfuran-3-yl)prop-2-en-1-one I [R = 2,5-(F)2-C6H3, 2-naphthyl, 2-biphenyl, etc.] were synthesized by using conventional and microwave irradiation methods in the presence of anhydrous potassium carbonate as an safe, inexpensive and efficient basic catalyst. Synthesized compounds were evaluated for their in-vitro antimicrobial activity against variety of microbial strains and it was characterized by IR, NMR (1H & 13C) and mass spectral anal. The biol. screening results indicated that some of the compounds showed significant antibacterial and antifungal activities. Compound I [R = 3-methyl-2-thiophenyl] displayed excellent antimicrobial activity against various microbial strains. The newly synthesized high potent compound I [R = 3-methyl-2-thiophenyl] was subjected to thermogravimetric anal. (TGA), differential scanning calorimetric (DSC) and single crystal XRD.

Pharma Chemica published new progress about Antibacterial agents. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, SDS of cas: 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Giri, T. published the artcileSynthesis and antibacterial activity of novel 4-{4-(methylamino)thieno[3,2-d]pyrimidin-2-yl}-benzohydrazide derivatives, Computed Properties of 71255-09-9, the main research area is methylaminothienopyrimidinyl benzohydrazide derivative preparation antibacterial agent.

A series of novel 4-{4-(methylamino)thieno[3,2-d]pyrimidin-2-yl}benzohydrazide derivatives were synthesized and evaluated for their antibacterial activity. Most of the compounds demonstrated high activity towards Escherichia coli, Pseudomonas, Staphylococcus aureus, and Bacillus. Structures of all synthesized compounds were confirmed by spectral anal.

Russian Journal of General Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Computed Properties of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Murphy, Rebecca A. published the artcileDirect Methoxypyridine Functionalization Approach to Magellanine-Type Lycopodium Alkaloids, Application of 2-Methoxynicotinaldehyde, the main research area is enantioselective synthesis tetracyclic core magellanine Lycopodium alkaloid; Hajos Parrish reaction enantioselective synthesis magellanine Lycopodium alkaloid; palladium catalyzed pyridine functionalization enantioselective synthesis magellanine Lycopodium alkaloid.

A concise enantioselective approach to the tetracyclic core of the magellanine-type Lycopodium alkaloids is reported. Key to this approach is the use of the Hajos-Parrish reaction to set a challenging quaternary stereocenter, thereby guiding the stereoselectivity for the remainder of the synthesis, as well as the use of a palladium-mediated direct pyridine functionalization reaction to forge the tetracyclic core.

Organic Letters published new progress about Alkaloids Role: SPN (Synthetic Preparation), PREP (Preparation) (Lycopodium). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application of 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Miura, Hiroki published the artcileRuthenium-Catalyzed Intermolecular Hydroacylation of Internal Alkynes: The Use of Ceria-Supported Catalyst Facilitates the Catalyst Recycling, HPLC of Formula: 71255-09-9, the main research area is conjugated enone preparation; ceria supported ruthenium hydroacylation alkyne aldehyde.

Intermol. hydroacylation of internal alkynes by aromatic aldehydes, catalyzed by Ru/CeO2 or [RuCl2(p-cymene)]2 in the presence of sodium formate and Xantphos, gave conjugated enones. E.g., in presence of Ru/CeO2, hydroacylation of PhCCPh by PhCHO gave 52% enone I (64:36 E/Z). The solid Ru/CeO2 continued to show catalytic activity and gave enones without significant decreases in yields for at least three times.

Chemistry – A European Journal published new progress about Alkynes, internal Role: RCT (Reactant), RACT (Reactant or Reagent). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, HPLC of Formula: 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rogers, David A. published the artcileAmplification of Trichloroisocyanuric Acid (TCCA) Reactivity for Chlorination of Arenes and Heteroarenes via Catalytic Organic Dye Activation, Recommanded Product: 2-Methoxynicotinaldehyde, the main research area is chlorination arene heteroarene trichloroisocyanuric acid brilliant green catalyst.

Heteroarenes and arenes that contain electron-withdrawing groups are chlorinated in good to excellent yields (scalable to gram scale) using trichloroisocyanuric acid (TCCA) and catalytic Brilliant Green (BG). Visible-light activation of BG serves to amplify the electrophilic nature of TCCA, providing a mild alternative approach to acid-promoted chlorination of deactivated (hetero)aromatic substrates. The utility of the TCCA/BG system is demonstrated through comparison to other chlorinating reagents and by the chlorination of pharmaceuticals including caffeine, lidocaine, and phenazone.

Organic Letters published new progress about Aryl chlorides Role: SPN (Synthetic Preparation), PREP (Preparation). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Recommanded Product: 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Savarimuthu, Sebastian Antony published the artcileSodium Tertiary Pentoxide as a Mild and Efficient Base to Make C-C Bond between Acetylenes and Aldehydes (or) Ketones Producing Propargyl Alcohols, COA of Formula: C7H7NO2, the main research area is carbonyl compound phenylacetylene sodium tertiary pentoxide promoter green coupling; propargyl alc preparation.

This report confirmed that sodium tertiary-pentoxide was a very effective base for the nucleophilic addition of acetylenes to aldehydes and ketones in 1,4-dioxane at room temperature These mild and operationally simple procedures were working well with a variety of aromatic and heteroaromatic aldehydes and also equally working well with aliphatic, aromatic and heteroaromatic ketones. A very clean product of secondary and tertiary propargylic alcs. were obtained from 70-94% yield. This process was explored in bulk scale synthesis on selected mols. and also adapted the column free purification for most of the substrates.

ChemistrySelect published new progress about Alcohols, propargyl Role: SPN (Synthetic Preparation), PREP (Preparation). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, COA of Formula: C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Choi, Ji Won published the artcileOptimization of vinyl sulfone derivatives as potent nuclear factor erythroid 2-related factor 2 (Nrf2) activators for Parkinson’s disease therapy, Computed Properties of 71255-09-9, the main research area is vinyl sulfone derivative Nrf2 activator Parkinson disease therapy.

We previously developed a novel series of vinyl sulfones as nuclear factor erythroid 2-related factor 2 (Nrf2) activators with therapeutic potential for Parkinson’s disease (PD). However, the previously developed lead compound (1) exhibited undesirable druglike properties. Here, we optimized vinyl sulfones by introducing nitrogen heterocycles to improve druglike properties. Among the synthesized compounds, 17e was the most promising drug candidate with good druglike properties. Compound 17e showed superior effects on Nrf2 activation in cell-based assays compared to compound 1 (17e: half-maximal effective concentration (EC50) = 346 nM; 1: EC50 = 530 nM). Compound 17e was further confirmed to induce expression of Nrf2-dependent antioxidant enzymes at both mRNA and protein levels. In a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced mouse model of PD, 17e significantly attenuated loss of tyrosine hydroxylase-immunopos. dopaminergic neurons, suppressed microglial activation, and alleviated PD-associated motor dysfunction. Thus, 17e is a novel Nrf2 activator with excellent druglike properties and represents a potential therapeutic candidate for PD.

Journal of Medicinal Chemistry published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (HO-1, expression induction). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Computed Properties of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem