70206-50-7

Usage

Structure

Pyridine ring attached to an aminoethyl group

Usage

Building block in the synthesis of pharmaceuticals and agrochemicals

Reactivity

High reactivity due to the presence of the pyridine ring and amino group

Versatility

Can be used in the production of specialty chemicals and materials

Biological activities

Potential as a chelating agent and anti-inflammatory properties

Applications

Chemical and pharmaceutical industries

Research interest

Ongoing scientific research into its properties and potential uses

Upstream product

• 872-85-5 pyridine-4-carbaldehyde 
• 141-43-5 ethanolamine 
• 54751-01-8 4-(bromomethyl)pyridine 
• 106782-22-3 2-{[1-Pyridin-4-yl-meth-(E)-ylidene]-amino}-ethanol 
• 106782-22-3 2-(4-pyridylmethylene amino) ethanol 

Downstream Products

• 1397956-80-7 5-(cyclohexylmethoxy)-3-(((2-hydroxyethyl)(pyridin-4-ylmethyl)amino)methyl)-4H-chromen-4-one 

Relevant academic research and scientific papers

NOVEL LYSOPHOSPHATIDIC ACID DERIVATIVE

PROBLEM TO BE SOLVED: To provide a compound that specifically activates an LPA4 receptor, and a pharmaceutical composition containing the same. SOLUTION: This invention relates to a novel lysophosphatidic acid derivative that has an agonistic action on an LPA4 receptor and is useful for the prevention and/or treatment of a disease with angiodysplasia caused by the LPA4 receptor, or a disease associated with angiopathy, or symptoms associated therewith. This invention also relates to a pharmaceutical composition containing the lysophosphatidic acid derivative. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT

Discovery of benzimidazole analogs as a novel interleukin-5 inhibitors

A series of novel hydroxyethylaminomethylbenzimidazole analogs 5a-y were synthesized and evaluated for their IL-5 inhibitory activity using pro-B Y16 cell line. Among them, 2-(((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)amino)butan-1-ol (5e, 94.3% inhibition at 30 μM, IC50 = 3.5 μM, cLogP = 4.132) and 3-cyclohexyl-2-(((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)amino) propan-1-ol (5k, 94.7% inhibition at 30 μM, IC50 = 5.0 μM, cLogP = 6.253) showed the most potent inhibitory activity. The essential feature of SAR (Fig. 5) indicated that the chromenone ring can be replaced by a benzimidazole ring to maintain the inhibitory activity. In addition, the hydroxyethylaminomethyl group was suitable for the IL-5 inhibitory activity. Moreover, the hydrophobic substituents on carbon play an important role in the IL-5 inhibitory activity of these analogs. However, N-substituted analogs did not improve inhibitory activity. In addition, MTT assay of 5e and 5k with normal B lymphoblasts revealed that they had no significant effects on cell viability.

Structural studies on bioactive compounds. 34.1 Design, synthesis, and biological evaluation of triazenyl-substituted pyrimethamine inhibitors of Pneumocystis carinii dihydrofolate reductase

The triazenyl-pyrimethamine derivative 3a (TAB), a potent and selective inhibitor of Pneumocystis carinii DHFR, was selected as the starting point for a lead optimization study. Molecular modeling studies, corroborated by a recent crystal structure determination of the ternary complex of P. carinii DHFR-NADPH bound to TAB, predicted that modifications to the acetoxy residue of the lead inhibitor could exploit binding opportunities in the vicinity of an active site pocket bounded by residues Ile33, Lys37, and Leu72. Substitutions in the benzyl moiety with electron-donating and electron-withdrawing groups were predicted to probe face-edge interactions with amino acid Phe69 unique to the P. carinii enzyme. New triazenes 10a-v and 12a-f were prepared by coupling the diazonium tetrafluoroborate salt 6b of aminopyrimethamine with substituted benzylamines or phenethylamines. The most potent of the new inhibitors against P. carinii DHFR was the naphthylmethyl-substituted triazene 10t (IC50: 0.053 μM), but a more substantial increase in potency against the rat liver DHFR led to a reduction in selectivity (ratio rat liver DHFR IC50/P. carinii DHFR IC50: 5.36) compared to the original lead structure 3a (ratio rat liver DHFR IC50/P. carinii DHFR IC50: 114).

HYDROGENATION OF 3,4-PYRIDYLIDENE AMINOETHANOLS AND FLOTATION PROPERTIES OF THE PRODUCTS OF THEIR REDUCTION

2-(Pyridylmethylene amino)ethanols A-(HOCH2CH2CH2N=CH)C5H4N were obtained by condensation of 3- and 4-pyridinealdehydes with monoethanolamine.IR and PMR spectra are quoted for the substances obtained, as well as data on their application in flotation of lead-zinc ore.By hydrogenation on Raney nickel at 65 deg C and 70 atm hydrogen pressure 2-(pyridylmethyl amino) ethanols A-(HOCH2CH2NHCH2)C5H4N were obtained.

Heterocyclic compounds

Novel insecticides of the formula STR1 in which n is 0 or 1, X is S, O, STR2 Y is N or STR3 Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R9 variously represent hydrogen or specified organic radicals.