74764-17-3

Usage

Uses

Used in Pharmaceutical Industry:
N-2-Pyridinyl-1,2-ethanediamine is used as a reactant for the synthesis of dual histamine H1 and H2 receptor antagonists based on cyanoguanidine. These antagonists are important in the development of medications that target histamine receptors, which play a crucial role in allergic reactions and other inflammatory processes.
Additionally, N-2-Pyridinyl-1,2-ethanediamine is used in the synthesis of 2-thiohydantoins as somatostatin receptor ligands. Somatostatin receptor ligands have potential applications in the treatment of various conditions, including neuroendocrine tumors and diabetes, by modulating the activity of somatostatin receptors.

InChI:InChI=1/C7H11N3/c8-4-6-10-7-3-1-2-5-9-7/h1-3,5H,4,6,8H2,(H,9,10)

Upstream product

• 109-04-6 2-bromo-pyridine 
• 107-15-3 ethylenediamine 
• 109-09-1 2-chloropyridine 
• 372-48-5 2-fluoropyridine 
• 90008-39-2 N-ethyl-N-[2]pyridyl hydrazine 
• 100-39-0 benzyl bromide 
• 504-29-0 2-aminopyridine 
• 141-43-5 ethanolamine 

Downstream Products

• 109912-28-9 N-(4-methoxybenzyl)-N-2-pyridinyl-1,2-ethanediamine 
• 109912-29-0 N'-formyl-N-(4-methoxybenzyl)-N-2-pyridinyl-1,2-ethanediamine 
• 109912-33-6 N-[2-[N-(4-methoxybenzyl)-N-(2-pyridyl)amino]ethyl]-N-methyl-6-aminohexanonitrile 
• 109912-35-8 7-({2-[(4-Methoxy-benzyl)-pyridin-2-yl-amino]-ethyl}-methyl-amino)-heptanenitrile 
• 109912-30-3 N-(4-methoxybenzyl)-N'-methyl-N'-(2-(N-phthalimido)ethyl)-N-2-pyridinyl-1,2-ethanediamine 
• 109912-31-4 2-[3-({2-[(4-Methoxy-benzyl)-pyridin-2-yl-amino]-ethyl}-methyl-amino)-propyl]-isoindole-1,3-dione 
• 3166-00-5 benzoylguanidine 
• 1353642-63-3 N₁-phenyl-N₂-(pyridin-2-yl)ethane-1,2-diamine 
• 1613269-50-3 ethyl 2-[4-[2-(2-pyridylamino)ethylamino]cyclohexyl]acetate 
• 1613269-96-7 ethyl 2-[4-[2-(2-pyridylamino)ethylamino]cyclohexyl]acetate 
• 149868-03-1 C₁₇H₂₃FN₄ 
• 109912-36-9 N-[2-[N-(4-methoxybenzyl)-N-(pyridin-2-yl)amino]ethyl]-N-methyl-1,2-ethanediamine 
• 1600520-47-5 C₁₅H₁₈FN₃ 
• 1600520-55-5 C₂₂H₂₉FN₄ 

Relevant academic research and scientific papers

INDOLE AHR INHIBITORS AND USES THEREOF

The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

Synthesis and RNA-Binding Properties of Extended Nucleobases for Triplex-Forming Peptide Nucleic Acids

Triple-helix formation, using Hoogsteen hydrogen bonding of triplex-forming oligonucleotides, represents an attractive method for sequence-specific recognition of double-stranded nucleic acids. However, practical applications using triple-helix-forming oligonucleotides and their analogues are limited to long homopurine sequences. The key problem for recognition of pyrimidines is that they present only one hydrogen-bond acceptor or donor group in the major groove. Herein, we report our first attempt to overcome this problem by using peptide nucleic acids (PNAs) modified with extended nucleobases that form three hydrogen bonds along the entire Hoogsteen edge of the Watson-Crick base pair. New nucleobase triples (five) were designed, and their hydrogen bonding feasibility was confirmed by ab initio calculations. PNA monomers carrying the modified nucleobases were synthesized and incorporated in short model PNA sequences. Isothermal titration calorimetry showed that these nucleobases had a modest binding affinity for their double-stranded RNA (dsRNA) targets. Finally, molecular modeling of the modified triples in PNA-dsRNA helix suggested that the modest binding affinity was caused by subtle structural deviations from ideal hydrogen-bonding arrangements or disrupted π-stacking of the extended nucleobase scaffolds.

Isoflavone amide type derivative, preparation method and medical application thereof

The invention relates to the field of medicinal chemistry, and relates to an isoflavone amide type derivative, a preparation method and a medical application thereof, in particular to an isoflavone amide type derivative with the general formula (I), a preparation method thereof, medicine compositions including the isoflavone amide type derivative and a medical application thereof, especially an application of the isoflavone amide type derivative as a medicine for preventing or curing hyperlipemia, obesity or type II diabetes. The general formula (I) is shown in the description.

Synthesis and dual histamine H1 and H2 receptor antagonist activity of cyanoguanidine derivatives

Premedication with a combination of histamine H1 receptor (H1R) and H2 receptor (H2R) antagonists has been suggested as a prophylactic principle, for instance, in anaesthesia and surgery. Aiming at pharmacological hybrids combining H1R and H2R antagonistic activity, a series of cyanoguanidines 14-35 was synthesized by linking mepyramine-type H1R antagonist substructures with roxatidine-, tiotidine-, or ranitidine-type H2R antagonist moieties. N-desmethylmepyramine was connected via a poly-methylene spacer to a cyanoguanidine group as the "urea equivalent" of the H2R antagonist moiety. The title compounds were screened for histamine antagonistic activity at the isolated ileum (H1R) and the isolated spontaneously beating right atrium (H2R) of the guinea pig. The results indicate that, depending on the nature of the H2R antagonist partial structure, the highest H1R antagonist potency resided in roxatidine-type compounds with spacers of six methylene groups in length (compound 21), and tiotidine-type compounds irrespective of the alkyl chain length (compounds 28, 32, 33), N-cyano-N'-[2-[[(2- guanidino-4-thiazolyl)methyl] thio]ethyl]-N″-[2-[N-[2-[N-(4-methoxybenzyl)-N-(pyridyl)-amino] ethyl]-N-methylamino]ethyl] guanidine (25, pKB values: 8.05 (H1R, ileum) and 7.73 (H2R, atrium) and the homologue with the mepyramine moiety connected by a six-membered chain to the tiotidine-like partial structure (compound 32, pKB values: 8.61 (H1R) and 6.61 (H2R) were among the most potent hybrid compounds. With respect to the development of a potential pharmacotherapeutic agent, structural optimization seems possible through selection of other H1R and H2R pharmacophoric moieties with mutually affinity-enhancing properties.

Synthesis of selectively mono-N-arylated aliphatic diamines via iridium-catalyzed amine alkylation

A highly selective phosphorus/nitrogen (P,N) ligand-based iridium catalyst system efficiently catalyzes the reaction of arylamines with unprotected amino alcohols, yielding N-arylated aliphatic diamines in yields of up to 93%. The reaction can be performe

Gemmacin B: Bringing diversity back into focus

Through the synthesis of a focused library and SAR investigations, a more potent analogue of gemmacin (discovered in a previous diversity-oriented synthesis (DOS) campaign), gemmacin B, was discovered. The Royal Society of Chemistry.

CATIONIC BACTERIOCHLOROPHYLL DERIVATIVES AND USES THEREOF

The invention provides cationic tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one positively charged group and/or at least one basic group that is converted to a positively charged group under physiological conditions, preferably Bchls having an onium group derived from a N-containing aliphatic or heterocyclic radical such as ammonium, guanidinium, imidazolium, pyridinium, and the like or a phosphonium, arsonium, oxonium, sulfonium, selenonium, telluronium, stibonium, or bismuthonium group, or a basic group that is converted to such onium groups under physiological conditions, said groups being bound to one or more of the positions 173, 133 and 32 of the Bchl molecule by ester or amide bond. The Bchls are useful for photodynamic therapy and diagnosis.

SUBSTITUTED 2H-[1,2,4]TRIAZOLO[4,3-A]PYRAZINES AS GSK-3 INHIBITORS

The invention relates to compounds of formula (I) prodrugs thereof, and the pahrmaceutically acceptabel salts of the compounds and prodrugs, wherein Ra, Rb, R1 and R2 are as defined herein; pharmaceutical compositions thereof; and uses thereof.

Substituted 4-amino[1,2,4]triazolo[4,3-a] quinoxalines

The present invention provides compounds of formula (I) the prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein Ra, Rb, R1, and R2 are as defined herein; pharmaceutical compositions thereof; and uses thereof.