Month: December 2022

Kawabata, Atsuhiko published the artcileEffects of anti-vertigo drugs on medial vestibular nucleus neurons activated by horizontal rotation, Recommanded Product: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate, the publication is Japanese Journal of Pharmacology (1991), 55(1), 101-6, database is CAplus and MEDLINE.

The effects of anti-vertigo drugs on the brain medial vestibular nucleus (MVN) neurons were examined to assess the site and mode of action using cats anesthetized with α-chloralose. Single neuron activity in the MVN was extracellularly recorded using a silver wire microelectrode filled with diphenhydramine, diphenidol, betahistine, glutamate, or NaCl. Type I of the MVN neurons were identified according to the responses obtained when the animal placed on a turn-table was rotated sinusoidally. The drug effects were examined on type I neurons which received impulses primarily from the labyrinth and sent them to the oculomotor nuclei. The microiontophoretic application of diphenhydramine, diphenidol, and betahistine inhibited the rotation-induced firing of type I MVN neurons. Diphenhydramine and diphenidol were more potent than betahistine. These drugs act directly on MVN neurons and reduce the responsiveness to rotatory stimulation.

Japanese Journal of Pharmacology 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, Recommanded Product: N-Methyl-2-(pyridin-2-yl)ethan-1-amine dimethanesulfonate.

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

Gavhane, Dinesh S. published the artcileNano Copper Catalyzed Microwave Assisted Coupling of Benzene Boronic Acids with Thiophenols, Category: pyridine-derivatives, the publication is Letters in Organic Chemistry (2019), 16(6), 491-494, database is CAplus.

A proficient, microwave mediated methodol. using CuFe₂O₄ nanoparticle as the catalyst for S-arylation of substituted benzene boronic acids with thiophenol was developed. In this method, the substituted thioethers were easily obtained through a C-S bond formation using microwave irradiation technique as well as conventional heating in the presence of CuFe₂O₄ nanoparticles with modest to excellent yields with the less reaction time. The ligand free microwave technique helped in the preparation of substituted thioethers in measurable amount within 10 mins. The same results were obtained with conventional heating in 12h. The reported method was economically efficient and an alternative to the initial existing method for the preparation of substituted thioethers.

Letters in Organic Chemistry 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 C5H6BNO2, Category: pyridine-derivatives.

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

Bagherzadeh, Nastaran published the artcileSustainable and recyclable magnetic nanocatalyst of 1,10-phenanthroline Pd(0) complex in green synthesis of biaryls and tetrazoles using arylboronic acids as versatile substrates, Application of 2-Pyridinylboronic acid, the publication is Molecular Catalysis (2021), 111489, database is CAplus.

A magnetic nanocatalyst was purveyed as a heterogeneous recoverable palladium-based catalyst anchored on green, sustainable and phosphine free support. Resulted Fe3O4@SiO2-Phen-Pd(0) nanocatalyst bearing powerful phenanthroline ligand was thoroughly characterized by physicochem. approaches like UV-vis, FT-IR, EDX, XRD, TGA, ICP, VSM, DLS, FESEM, and TEM analyses. After finding trustable data, the obtained magnetic catalyst was considered to be applied in the Suzuki-Miyaura type C-C couplings and getting corresponding tetrazoles using arylboronic acid derivatives as alternate precursors of aromatic halides and stupendous data were observed

Molecular Catalysis 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 C5H6BNO2, Application of 2-Pyridinylboronic acid.

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

Schaffner, Arnaud-Pierre published the artcilePhosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa), Application of 2-Pyridinylboronic acid, the publication is Journal of Medicinal Chemistry (2021), 64(7), 3897-3910, database is CAplus and MEDLINE.

Selective and potent inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) have the potential to increase endogenous and therapeutic fibrinolysis and to behave like profibrinolytic agents without the risk of major hemorrhage, since they do not interfere either with platelet activation or with coagulation during blood hemostasis. Therefore, TAFIa inhibitors could be used in at-risk patients for the treatment, prevention, and secondary prevention of stroke, venous thrombosis, and pulmonary embolisms. In this paper, we describe the design, the structure-activity relationship (SAR), and the synthesis of novel, potent, and selective phosphinanes and azaphosphinanes as TAFIa inhibitors. Several highly active azaphosphinanes display attractive properties suitable for further in vivo efficacy studies in thrombosis models.

Journal of Medicinal Chemistry 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 C5H6BNO2, Application of 2-Pyridinylboronic acid.

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

Filace, Fabiana published the artcileSilyl Assistance in the Intramolecular Addition of Pyridyl Radicals onto Pyridines and Quinolines, Quality Control of 39856-58-1, the publication is European Journal of Organic Chemistry (2016), 2016(10), 1891-1896, database is CAplus.

The first example of a stable acylazinium salt obtained by an intramol. acylpyridine-centered radical attack on azine nitrogen atoms is reported. Depending on the relative position of the bromo substituent on the attacking aminopyridine ring, it is possible to obtain selectively either the N-attack product or a different C-attack derivative A rationale for this pathway selectivity was obtained from quantum mech. calculations

European Journal of Organic 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, Quality Control of 39856-58-1.

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

Narimani, Saeedeh published the artcileMicrowave-assisted facile synthesis of N, P co-doped fluorescent carbon dot probe for the determination of nifedipine., Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Analytical sciences : the international journal of the Japan Society for Analytical Chemistry (2022), 38(2), 393-399, database is MEDLINE.

A simple and fast microwave synthesis method was applied for the preparation of several carbon dots (CDs) from various combinations of urea, phosphoric acid, and B-alanine as nitrogen, phosphorus, and carbon precursors. The maximum quantum yield (44%) was obtained for nitrogen and phosphorus co-doped carbon dots (N, P-CDs) prepared from urea, B-alanine, and phosphoric acid. Furthermore, N, P-CDs were exploited to synthesize a simple and sensitive fluorometric probe to determine nifedipine (NFD). We determined that the analytical response of the designed sensor could be affected by the kind of dopant and synthesis precursors. It is worth mentioning that the fluorescence intensity of N, P-CDs was weakened by NFD, and no fluorescence quenching was observed for other prepared CDs. The NFD-developed sensor demonstrated a linear response range of 3.3 ×â€?0^-8-3.2 ×â€?0^-5 mol/L, with the detection limit of 1.0 ×â€?0^-8 mol/L. The sensor was successfully applied to measure NFD in human biological fluids.

Analytical sciences : the international journal of the Japan Society for Analytical Chemistry 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, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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

Heinrich, Timo published the artcileDiscovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology, Application of 2-Bromopyridin-3-amine, the publication is Journal of Medicinal Chemistry (2021), 64(16), 11904-11933, database is CAplus and MEDLINE.

Due to increased lactate production during glucose metabolism, tumor cells heavily rely on efficient lactate transport to avoid intracellular lactate accumulation and acidification. Monocarboxylate transporter 4 (MCT4/SLC16A3) is a lactate transporter that plays a central role in tumor pH modulation. The discovery and optimization of a novel class of MCT4 inhibitors (hit 9a), identified by a cellular screening in MDA-MB-231, is described. Direct target interaction of the optimized compound 18n with the cytosolic domain of MCT4 was shown after solubilization of the GFP-tagged transporter by fluorescence cross-correlation spectroscopy and microscopic studies. In vitro treatment with 18n resulted in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. Moreover, pharmacokinetic properties of 18n allowed assessment of lactate modulation and antitumor activity in a mouse tumor model. Thus, 18n represents a valuable tool for investigating selective MCT4 inhibition and its effect on tumor biol.

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, Application of 2-Bromopyridin-3-amine.

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

Taya, Toshiki published the artcileComplexation behavior of heterocyclic hydrazones. I. Structure and acid-base equilibria for heterocyclic hydrazones, Application In Synthesis of 2215-33-0, the publication is Bulletin of the Chemical Society of Japan (1993), 66(12), 3652-61, database is CAplus.

The acid-base equilibrium of twenty-one hydrazones substituted by Ph, pyridyl and/or quinolyl groups have been investigated in aqueous solutions over the region of H_– to H₀ acidity function by a spectrophotometric method at 25 °C. For 2-pyridinecarbaldehyde 2-(5-substituted)pyridylhydrazones, although the proton dissociation of the neutral species (HL) satisfied a Hammett correlation, those of H₂L⁺ and H₃L²⁺ did not. The thermodn. parameters for the proton dissociations of H₂L⁺ of seven representative ligands were determined by a temperature-coefficient method at 25 °C and an ionic strength of 0.1 (KCl). The enthalpy and entropy changes for the proton dissociations of H₃L²⁺ and H₂L⁺ were influenced by the steric effects of the Me group and/or the introduced quinolyl ring. An anal. of the pH dependence of the ¹H NMR signals for three hydrazones in an acetone-d₆-D₂O solution gave more profitable information concerning the fine structures of HL, H₂L⁺, and H₃L²⁺. Each ¹H and ¹³C NMR chem. shift of some ring-substituted Me derivatives (HL form) in a dioxane-D₂O solution has been briefly assigned. On the other hand, a single-crystal X-ray anal., ¹H NMR data in chloroform-d and thermodn. data for di-2-pyridyl ketone 2-pyridylhydrazone (DPPH) suggested that the intramol. hydrogen bond in the DPPH mol. is broken by the addition of a proton on the H₂L⁺ species in an aqueous solution

Bulletin of the Chemical Society of Japan published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C10H10O2, Application In Synthesis of 2215-33-0.

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

Odashima, Tsugikatsu published the artcileSynthesis and properties of 3-, 4-, and 5-nitro-2-pyridinecarboxaldehyde 2-pyridylhydrazones and characterization of their metal complexes, Synthetic Route of 2215-33-0, the publication is Bulletin of the Chemical Society of Japan (1993), 66(3), 797-803, database is CAplus.

Three title hydrazones (I, R = 3-, 4-, and 5-NO₂), were synthesized. Their properties and reactivities with metal ions and the extraction and characteristics of the resultant complexes were investigated and compared with one another. As a result, useful information on the mol. design of highly sensitive hydrazone reagents was obtained.

Bulletin of the Chemical Society of Japan published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C11H10N4, Synthetic Route of 2215-33-0.

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

Joseph, Jayan T. published the artcileAryl/heteroaryl pentafluorobenzenesulfonates (ArOPFBs): new electrophilic coupling partners for room temperature Suzuki-Miyaura cross-coupling reactions, HPLC of Formula: 1008506-24-8, the publication is Tetrahedron Letters (2015), 56(36), 5106-5111, database is CAplus.

The first Suzuki-Miyaura cross-coupling reaction between aryl pentafluorobenzenesulfonates e.g., I, and aryl boronic acids under mild conditions was described. High chemoselectivity of these bench stable aryl pentafluorobenzenesulfonates over tosylates, triflates, mesylates, and chlorides for the successful synthesis of highly ortho substituted biaryls was also discussed. Addnl., the generality of this protocol was further extended to other boron containing nucleophiles (boronates, trifluoroborates) and alkyl boronic acids. This process had several advantages which include use of mild catalyst, rapid reaction conditions, wide substrate scope, facile synthesis and high chemoselectivity with good yields.

Tetrahedron Letters published new progress about 1008506-24-8. 1008506-24-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Pyridine,Boronic Acids,Boronic acid and ester, name is 3-Methoxypyridine-4-boronic acid, and the molecular formula is C6H8BNO3, HPLC of Formula: 1008506-24-8.

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