Day: December 7, 2022

Ojha, K. G. published the artcileSynthesis and antibacterial activity of some substituted phenothiazin-3-ones, Related Products of pyridine-derivatives, the publication is International Journal of Chemical Sciences (2003), 1(4), 347-350, database is CAplus.

1,2,4-Trihalophenothiazin-3-ones were prepared by condensing 2-aminobenzenethiols with chloranil/bromanil in 1:1 molar ratio. These compounds on refluxing with aryl amine and anhydrous NaOAc in EtOH gave substituted 2-arylaminophenothiazin-3-ones, which exhibited antibacterial activity.

International Journal of Chemical Sciences published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Related Products of pyridine-derivatives.

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

Decristoforo, Clemens published the artcile99M-technetium-labelled peptide-HYNIC conjugates: Effects of lipophilicity and stability on biodistribution, Computed Properties of 636-73-7, the publication is Nuclear Medicine and Biology (1999), 26(4), 389-396, database is CAplus and MEDLINE.

The aim of this study was to explore the effects of lipophilicity and stability on the biodistribution of ^99mTc labeled peptides through the use of different co-ligands. 6-Hydrazinopyridine-3-carboxylic acid (HYNIC) was coupled to the somatostatin analog RC160 and radiolabeled using a range of ethylenediaminediacetic acid (EDDA) and EDTA derivatives as well as tricine and pyridine/tricine as co-ligands. After labeling with technetium-99m, chromatog., stability, protein-binding, and rat biodistribution studies were performed. For most co-ligands, biodistribution correlated well with in vitro properties. Lipophilic substitution on EDDA resulted in higher protein binding, increased liver uptake, and intestinal excretion. Stabilization of tricine with pyridines reduced blood levels and lowered liver uptake. EDTA derivatives showed high instability in vitro and in vivo.

Nuclear Medicine and Biology 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, Computed Properties of 636-73-7.

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

Brunner, Katharina published the artcileInhibitors of the Cysteine Synthase CysM with Antibacterial Potency against Dormant Mycobacterium tuberculosis, SDS of cas: 197958-29-5, the publication is Journal of Medicinal Chemistry (2016), 59(14), 6848-6859, database is CAplus and MEDLINE.

Cysteine is an important amino acid in the redox defense of Mycobacterium tuberculosis, primarily as a building block of mycothiol. Genetic studies have implicated de novo cysteine biosynthesis in pathogen survival in infected macrophages, in particular for persistent M. tuberculosis. Here, we report on the identification and characterization of potent inhibitors of CysM, a critical enzyme in cysteine biosynthesis during dormancy. A screening campaign of 17,312 compounds identified ligands that bind to the active site with micromolar affinity. These were characterized in terms of their inhibitory potencies and structure-activity relationships through hit expansion guided by three-dimensional structures of enzyme-inhibitor complexes. The top compound binds to CysM with 300 nM affinity and displays selectivity over the mycobacterial homologues CysK1 and CysK2. Notably, two inhibitors show significant potency in a nutrient-starvation model of dormancy of Mycobacterium tuberculosis, with little or no cytotoxicity toward mammalian cells.

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, SDS of cas: 197958-29-5.

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

Lauro, Figueroa-Valverde published the artcileSynthesis and Biological Activity of the Pyridine-hexacyclic-steroid Derivative on a Heart Failure Model., Computed Properties of 21829-25-4, the publication is Anti-inflammatory & anti-allergy agents in medicinal chemistry (2022), 21(1), 34-45, database is MEDLINE.

BACKGROUND: Several drugs with inotropic activity have been synthesized; however, there is very little information on biological activity exerted by steroid derivatives in the cardiovascular system. OBJECTIVE: The aim of this research was to prepare a steroid-pyridine derivative to evaluate the effect it exerts on left ventricular pressure and characterize its molecular interaction. METHODS: The first stage was carried out through the synthesis of a steroid-pyridine derivative using some chemical strategies. The second stage involved the evaluation of the biological activity of the steroid-pyridine derivative on left ventricular pressure using a model of heart failure in the absence or presence of the drugs, such as flutamide, tamoxifen, prazosin, metoprolol, indomethacin, and nifedipine. RESULTS: The results showed that steroid-pyridine derivative increased left ventricular pressure in a dose-dependent manner (0.001-100 nM); however, this phenomenon was significantly inhibited only by nifedipine at a dose of 1 nM. These results indicate that positive inotropic activity produced by the steroid-pyridine derivative was via calcium channel activation. Furthermore, the biological activity exerted by the steroid-pyridine derivative on the left ventricle produces changes in cAMP concentration. CONCLUSION: It is noteworthy that positive inotropic activity produced by this steroid-pyridine derivative involves a different molecular mechanism compared to other positive inotropic drugs. Therefore, this steroid could be a good candidate for the treatment of heart failure.

Anti-inflammatory & anti-allergy agents in medicinal 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, Computed Properties of 21829-25-4.

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

Kantak, Abhishek A. published the artcileRegioselective C-H bond amination by aminoiodanes, Category: pyridine-derivatives, the publication is Chemical Communications (Cambridge, United Kingdom) (2015), 51(17), 3574-3577, database is CAplus and MEDLINE.

A new approach for the direct amination of 2-phenylpyridine derivatives using a diphthalimide-iodane and copper triflate has been developed. A series of different 2-phenylpyridine derivatives were aminated with yields up to 88%. Mechanistic investigations indicate that the reaction proceeds via a copper-mediated single electron transfer.

Chemical Communications (Cambridge, United Kingdom) published new progress about 89076-64-2. 89076-64-2 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitro Compound,Benzene, name is 5-Nitro-2-phenylpyridine, and the molecular formula is C11H8N2O2, Category: pyridine-derivatives.

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

Grases, F. published the artcileDetermination of cobalt(II) by use of a very simple monitored thermometric technique based on the action of this cation on the aerial oxidation of 2,2′-dipyridyl ketone hydrazone, Quality Control of 2215-33-0, the publication is Journal of Thermal Analysis (1984), 29(6), 1397-402, database is CAplus.

Co(II) 0.1-0.9 ppm was determined by catalysis of autoxidation of 1.0mM di(2-pyridyl) ketone hydrazone at pH 12 (Clark-Lubs buffer), monitored by thermometry. The relative standard deviation was 2.1%. The selectivity was good.

Journal of Thermal Analysis 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, Quality Control of 2215-33-0.

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

Grases, F. published the artcileFluorometric reaction-rate method for determination of mercury with 2,2′-dipyridyl ketone hydrazone, Name: 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, the publication is Microchemical Journal (1985), 32(3), 367-72, database is CAplus.

A simple and sensitive fluorometric reaction-rate method for determination of Hg(II) (0.03-0.3 ppm), based on its catalytic effect on the autoxidation of 2,2′-dipyridyl ketone hydrazone, was developed. The reaction is followed by the measurement of the rate of appearance of the blue fluorescence (λ_ex = 359, λ_em = 430 nm). The exptl. variables and interferences in the determination are also reported.

Microchemical Journal 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, Name: 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine.

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

Grases, F. published the artcileReactions between technetium(VII) and some hydrazones and the spectrofluorometric determination of technetium(VII) with 2,2′-dipyridyl ketone hydrazone, Product Details of C11H10N4, the publication is Analytica Chimica Acta (1984), 71-8, database is CAplus.

The reactions between pertechnetate and 5 hydrazones are described. Of these, the Tc(VII)/2,2′-dipyridyl ketone hydrazone system was found to be most sensitive, and was studied in detail. Spectrofluorometric procedures for the determination of Tc(VII) over the range 0.01-12 mg L^-1 are reported. The reaction proceeds most favorably under acidic conditions (1.4M HCl). For 1 mg L^-1 Tc(VII), 100 mg L^-1 levels of U(VI), Re(VII), Mo(VI), or W(VI) do not interfere when the reaction proceeds at room temperature Sensitivity improves at higher temperatures

Analytica Chimica Acta 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, Product Details of C11H10N4.

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

Hou, Zhong-Wei published the artcileElectrochemical Synthesis of Polycyclic N-Heteroaromatics through Cascade Radical Cyclization of Diynes, Recommanded Product: 2-Bromopyridin-3-amine, the publication is ACS Catalysis (2017), 7(9), 5810-5813, database is CAplus.

An electrochem. cyclization reaction of easily available urea-tethered diynes was developed for the synthesis of N-doped polycyclic aromatic hydrocarbons (PAHs). The employment of ferrocene as a mild and selective redox catalyst allows access to a variety of electron-rich PAHs including helicene-like structures without overoxidn. The electrosynthetic method involves an unprecedented amidyl radical cascade cyclization process to form three rings in a single operation.

ACS Catalysis 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, Recommanded Product: 2-Bromopyridin-3-amine.

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

Zhang, Xudong published the artcileHergSPred: Accurate Classification of hERG Blockers/Nonblockers with Machine-Learning Models, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Journal of Chemical Information and Modeling (2022), 62(8), 1830-1839, database is CAplus and MEDLINE.

The human ether-á-go-go-related gene (hERG) K+ channel plays an important role in cardiac action potentials. The inhibition of the hERG channel may lead to long QT syndrome (LQTS) and even sudden cardiac death. Due to severe hERG-related cardiotoxicity, many drugs have been withdrawn from the market. Therefore, it is necessary to estimate the chem. blockade of hERG in the early stage of drug discovery. In this study, we collected 12,850 compounds with hERG inhibition data from the literature and trained a series of hERG blocking classification models based on the MACCS and Morgan fingerprints. A consensus model named HergSPred was generated based on the individual models using voting principles. The accuracy of HergSPred is higher than previous models using identical training and test sets. Moreover, we analyzed the contribution of each input fingerprint to the prediction output to obtain intuitive chem. insights into the hERG inhibition, which allows visualization of warning substructures that may cause cardiotoxicity in the input compound The model is available at http://www.icdrug.com/ICDrug/T.

Journal of Chemical Information and Modeling 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 C17H37NO3, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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