Category: pyridine-derivatives

Yang, Lei published the artcilePalladium(0)-catalyzed asymmetric C(sp³)-H arylation using a chiral binol-derived phosphate and an achiral ligand, Recommanded Product: 2-Bromopyridin-3-amine, the publication is Chemical Science (2017), 8(2), 1344-1349, database is CAplus and MEDLINE.

The first efficient palladium(0)-catalyzed enantioselective C(sp³)-H activation reaction using a catalytic chiral base and an achiral phosphine ligand was reported. Fine-tuning the binol-derived phosphoric acid pre-catalyst and the reaction conditions was found to be crucial to achieve high levels of enantioselectivity for a variety of indoline products containing both tri- and tetrasubstituted stereocenters.

Chemical Science published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C16H20N2, Recommanded Product: 2-Bromopyridin-3-amine.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Souza de Araujo, Guilherme Rodolfo published the artcileMicroemulsions formed by PPG-5-CETETH-20 at low concentrations for transdermal delivery of nifedipine: Structural and in vitro study, Application In Synthesis of 21829-25-4, the publication is Colloids and Surfaces, B: Biointerfaces (2022), 112474, database is CAplus and MEDLINE.

Nifedipine is a potent anti-hypertensive, which is poorly orally bioavailable on account of first-pass metabolism, short half-life, and low water solubility This study aimed to develop a microemulsified system with low surfactant concentration and to evaluate the influence of microemulsion (ME) phase behavior on skin permeation of nifedipine, as drug model. Thereafter, MEs were obtained using PPG-5-CETETH-20, oleic acid, and phosphate buffer at pH 5.0. The selected MEs were isotropic, with droplet diameters less than 10 nm, polydispersity index < 0.25, and pH between 5.0 and 5.2. MEs presented low viscosity and Newtonian behavior. SAXS results confirmed bicontinuous and oil-in-water (o/w) MEs formation. The presence of the drug promoted only very slight modifications in the ME structure. The MEs presented ability to deliver nifedipine via the transdermal route when in comparison with the control. Nevertheless, the skin permeated and retained amounts from the o/w and bicontinuous formulations did not differ significantly. The ATR-FTIR demonstrated that both formulations promoted fluidization and disorganization of lipids and increased the drug diffusion and partition coefficients in the skin. In conclusion, PPG-5-CETETH-20 MEs obtained proved to be effective skin permeation enhancers, acting by rising the coefficients of partition and diffusion of the nifedipine in the skin.

Colloids and Surfaces, B: Biointerfaces published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C15H14N2, Application In Synthesis of 21829-25-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Hoepping, Alexander published the artcileAn alternative synthesis of sodium cyanodithioformate and the disodium salt of cis-1,2-dicyanoethylene-1,2-dithiol, Category: pyridine-derivatives, the publication is Journal fuer Praktische Chemie/Chemiker-Zeitung (1998), 340(3), 269-270, database is CAplus.

A new synthesis of Na cyanodithioformate and the disodium salt of cis-1,2-dicyanoethylene-1,2-dithiol is reported. The key step involves a nucleophilic thiolation with elemental S starting from a substituted acetonitrile. This method may serve as a cyanide- and CS₂-free alternative in the preparation of the title compounds

Journal fuer Praktische Chemie/Chemiker-Zeitung published new progress about 17281-59-3. 17281-59-3 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitrile,Salt, name is 1-(Cyanomethyl)pyridin-1-ium chloride, and the molecular formula is C7H7ClN2, Category: pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Galli, Ubaldina published the artcileIdentification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2, Application of Pyridine-3-sulfonic acid, the publication is European Journal of Medicinal Chemistry (2012), 58-66, database is CAplus and MEDLINE.

As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogs of nicotinamide. Biol. data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.

European Journal of Medicinal Chemistry published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, Application of Pyridine-3-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Yin, Xiaojun published the artcileStar-Shaped Macromolecules with the Core of Hexakis-(fluoren-2-yl)benzene and the Periphery of Pyridine: Synthesis and Application as Solution-Processable Electron-Transport Materials, COA of Formula: C5H6BNO2, the publication is Macromolecular Rapid Communications (2015), 36(18), 1658-1663, database is CAplus and MEDLINE.

Three new star-shaped macromols. with hexakis(fluoren-2-yl)benzene as the core and pyridine as the periphery (2Py-HFB, 3Py-HFB, and 4Py-HFB) are synthesized and characterized. The synthetic conditions of octacarbonyldicobat-catalyzed cycloaddition reaction for different alkyne precursors are investigated. The coordination interaction between the pyridine ring of alkyne precursor and the cobalt catalyst may result in very low yield of the cyclotrimerization product. However, with the increase of the catalyst loading, the yields of the intermediates of cyclopentadienone are enhanced. Then, the desired cyclotrimerization products can be obtained by the Diels-Alder reactions of cyclopentadienone with acetylene in good yield. These new compounds exhibit good thermal stability and favorable electron affinity. By using the new compounds as electron-transporting materials, all-solution-processed phosphorescent organic light-emitting devices (OLEDs) show good performance with a maximum current efficiency of 5.6 cd A^-1 and maximum external quantum efficiency of 4.68%.

Macromolecular Rapid Communications published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C14H10N2O, COA of Formula: C5H6BNO2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Krow, Grant published the artcileReinvestigation of 1,2-dihydropyridine formation by condensation of aldehydes with aniline. Revision of a structural assignment, Formula: C18H25N, the publication is Tetrahedron Letters (1971), 3653-6, database is CAplus.

The product of the HOAc catalyzed condensation of 3:1 PrCHO-PhNH2 was established by uv and NMR spectra as I. The reaction of I with maleic anhydride gave II, via a concerted π2s+π4s addition The structure and stereochemistry of II was determined by its NMR spectrum in the presence of Eu(DPM)3. In this abstract DPM=(tert-BuCO)2C-H.

Tetrahedron Letters published new progress about 34562-31-7. 34562-31-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is 3,5-Diethyl-1-phenyl-2-propyl-1,2-dihydropyridine, and the molecular formula is C18H25N, Formula: C18H25N.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Nevskaya, Alisa A. published the artcileSynthesis and cytotoxicity of novel 1-arylindolizines and 1-arylpyrrolo[2,1-a]isoquinolines, Product Details of C12H9NO, the publication is Tetrahedron Letters (2021), 153552, database is CAplus.

An efficient approach to the synthesis of indolizines and pyrrolo[2,1-a]isoquinolines based on a domino reaction was described. The reactivity of the derivatives and the structure-activity anal. are carried out in a number of the obtained compounds A hit was found showing high cytotoxicity on tumor cells whose cytotoxic effect was comparable to that of the known topoisomerase I inhibitor camptothecin.

Tetrahedron Letters published new progress about 91-02-1. 91-02-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene,Ketone, name is Phenyl(pyridin-2-yl)methanone, and the molecular formula is C12H9NO, Product Details of C12H9NO.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Kowol, Christian R. published the artcileImpact of Stepwise NH₂-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention, Safety of 2-Bromopyridin-3-amine, the publication is Journal of Medicinal Chemistry (2016), 59(14), 6739-6752, database is CAplus and MEDLINE.

One of the most promising classes of iron chelators are α-N-heterocyclic thiosemicarbazones with Triapine as the most prominent representative. In several clin. trials Triapine showed anticancer activity against hematol. diseases, however, studies on solid tumors failed due to widely unknown reasons. Some years ago, it was recognized that “terminal dimethylation” of thiosemicarbazones can lead to a more than 100-fold increased activity, probably due to interactions with cellular copper depots. To better understand the structural requirements for the switch to nanomolar cytotoxicity, we systematically synthesized all eight possible N-methylated derivatives of Triapine and investigated their potential against Triapine-sensitive as well as -resistant cell lines. While only the “completely” methylated compound exerted nanomolar activity, the data revealed that all compounds with at least one N-dimethylation were not affected by acquired Triapine resistance. In addition, these compounds were highly synergistic with copper treatment accompanied by induction of reactive oxygen species and massive necrotic cell death.

Journal of Medicinal Chemistry published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Safety of 2-Bromopyridin-3-amine.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Nishide, Shigenori published the artcileImproved determination of betahistine mesylate, Synthetic Route of 54856-23-4, the publication is Yakugaku Zasshi (1983), 103(11), 1180-4, database is CAplus and MEDLINE.

An improved method for the determination of betahistine mesylate (I) [54856-23-4] in tablets was developed by the use of UV spectrophotometry at 260 nm. The determination of in aqueous solutions were affected by pH and temperature The measurement of the mesylate in 0.1 N sulfuric acid instead of water produced more accurate results.

Yakugaku Zasshi published new progress about 54856-23-4. 54856-23-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Salt,Amine,Inhibitor,Inhibitor, name is N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, and the molecular formula is C10H20N2O6S2, Synthetic Route of 54856-23-4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Michiba, Kazuyoshi published the artcileUsefulness of human jejunal spheroid-derived differentiated intestinal epithelial cells for the prediction of intestinal drug absorption in humans, Product Details of C17H18N2O6, the publication is Drug Metabolism & Disposition (2022), 50(3), 204-213, database is CAplus and MEDLINE.

This study aimed to demonstrate the usefulness of human jejunal spheroid-derived differentiated intestinal epithelial cells as a novel in vitro model for clarifying the impact of intestinal drug-metabolizing enzymes and transporters on the intestinal absorption of substrate drugs in humans. Three-dimensional human intestinal spheroids were successfully established from surgical human jejunal specimens and expanded for a long period using L-WRN-conditioned medium, which contains Wnt3a, R-spondin 3, and noggin. The mRNA expression levels of intestinal pharmacokinetics-related genes in the human jejunal spheroid-derived differentiated intestinal epithelial cells were drastically increased over a 5-day period after seeding compared with those in human jejunal spheroids and were approx. the same as those in human jejunal tissue over a culture period of at least 13 days. Activities of typical drug-metabolizing enzymes [cytochrome P 450 (CYP) 3A, CYP2C9, uridine 5-diphospho-glucuronosyltransferase 1A, and carboxylesterase 2] and uptake/efflux transporters [peptide transporter 1/solute carrier 15A1], P-glycoprotein, and breast cancer resistance protein) in the differentiated cells were confirmed. Furthermore, intestinal availability (Fg) values estimated from the apical-to-basolateral permeation clearance across cell monolayer showed a good correlation with the in vivo Fg values in humans for five CYP3A substrate drugs (Fg range, 0.35-0.98). In conclusion, the functions of major intestinal drug-metabolizing enzymes and transporters could be maintained in human jejunal spheroid-derived differentiated intestinal epithelial cells. This model would be useful for the quant. evaluation of the impact of intestinal drug-metabolizing enzymes and transporters on the intestinal absorption of substrate drugs in humans.

Drug Metabolism & Disposition published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem