102127-29-7

Upstream product

• 37699-43-7 2,3-dimethyl-4-nitropyridine N-oxide 
• 100-51-6 benzyl alcohol 
• 22710-07-2 2,3-dimethylpyridine 1-oxide 
• 583-61-9 2,3-Lutidine 
• 59886-90-7 4-chloro-2,3-dimethylpyridine-N-oxide 

Downstream Products

• 1029128-23-1 4-(benzyloxy)-6-chloro-2,3-dimethylpyridine 
• 102127-30-0 Acetic acid 4-benzyloxy-3-methyl-pyridin-2-ylmethyl ester 
• 768319-30-8 4-Benzyloxy-2-chloromethyl-3-methyl-pyridine 
• 102137-66-6 (4-Benzyloxy-3-methyl-pyridin-2-yl)-methanol 

Relevant academic research and scientific papers

ARYL HYDROCARBON RECEPTOR LIGANDS AND THEIR ANALOGUES FOR THE PREVENTION AND TREATMENT OF INFLAMMATORY DISORDERS

Aryl hydrocarbon receptor (AHR) agonists and their use in treating or preventing or reducing the risk of an inflammatory disorder associated with a reduced expression of an aryl hydrocarbon receptor (AHR), including necrotizing enterocolitis, for preventing, reducing the risk of, or reducing the severity of an inflammatory disorder associated with a reduced expression of an aryl hydrocarbon receptor (AHR), and as an additive to infant nutritional formulas.

Preparation method of rabeprazole sodium impurity

The invention discloses a synthesizing method of a rabeprazole sodium impurity, and belongs to the field of medicine synthesis. A preparation method has the advantages that the technology design is reasonable, the operability is strong, the reaction conditions are more moderate, the yield rate is high, and the industrialization production is realized. The preparation method is characterized in that 2,3-dimethyl-4-chloropyridine-N-oxide and 2-chlorobenzimidazole are used as raw materials, and the eight-step reaction is performed, so as to realize the synthesis of the rabeprazole sodium impurity. The prepared rabeprazole sodium impurity has the advantages that the important basis is provided for the scientific evaluation on quality, safety and efficiency of rabeprazole sodium; the pharmacological activity of the rabeprazole sodium impurity is good; the medicines for treating active duodenal ulcer, benign gastric ulcer and duodenal ulcer with positive helicobacter pylori due to various reasons can be developed, and the important application value is realized.

PYRIDINE COMPOUNDS AND METHODS OF THEIR USE

Novel pyridine compounds, pharmaceutical compositions containing the pyridine compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the pyridine compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.

Structure-activity relationship of 2-[[(2-Pyridyl)methyl]thio]-1H- benzimidazoles as anti Helicobacter pylori agents in vitro and evaluation of their in vivo efficacy

A relationship between the structure of 21 2-[[(2-pyridyl)methyl]thio]- 1H-benzimidazoles (6) and their anti Helicobacter pylori activity expressed as minimum bactericidal concentration (MBC) values is described. Observed MBCs ranged from 256 to 1 μg/mL. The structure - activity relationship (SAR) showed that larger and more lipophilic compounds, especially compounds with such substituents in the 4-position of the pyridyl moiety, generally had lower MBC values. Four new compounds 'that were predicted to be potent by the established SAR model were synthesized and tested. One such compound, i.e., 2-[[(4-[(cyclopropylmethyl)oxy]3-methyl-2-pyridyl)methyl]thio]-1H- benzimidazole (18), was tested for in vivo efficacy in a mouse Helicobacter felis model (125 μmol/kg bid given orally for 4 days, n = 4). Unfortunately, antibacterial activity could not be clearly demonstrated in this model. Instead a potent acid secretion inhibition was observed. This finding was attributed to the methylthio compound being oxidized to the corresponding methyl sulfinyl derivative, i.e., a proton pump inhibitor, in vivo. Although the antibacterial activity had the potential of decreasing H. felis cell counts in vivo the proton pump inhibitory effect became dominant and actually promoted H. felis cell growth. Hence, we conclude that the antibacterial utility of the 2-[[(2-pyridyl)methyl]thio]1H-benzimidazoles (6) as a compound class is compromised by their propensity to become proton pump inhibitors upon metabolic oxidation in vivo.