Day: December 9, 2022

Yamada, Mamoru published the artcileMicrobial conversion of 5-sulfoisophthalic acid into 5-hydroxyisophthalic acid by Ochrobactrum anthropi S9, Related Products of pyridine-derivatives, the publication is Biotechnology Letters (2010), 32(3), 445-450, database is CAplus and MEDLINE.

5-Hydroxyisophthalic acid-producing microorganisms were isolated from enrichment cultures using 5-sulfoisophthalic acid as a sulfur source. One bacterium, Ochrobactrum anthropi S9, had the highest 5-sulfoisophthalic acid-degrading activity, and stoichiometrically formed 5-hydroxyisophthalic acid, a raw material for polymer synthesis. Under optimum culture conditions, 1.3 mM 5-hydroxyisophthalic acid accumulated in the medium by 60 h. The addition of Na₂SO₄, l-methionine or l-cysteine at 2 mM inhibited the conversion of 5-sulfoisophthalic acid. O. anthropi S9 cells converted 5-sulfoisophthalic acid, benzenesulfonic acid, 3-sulfobenzoic acid, 4-aminobenzenesulfonic acid, naphthalene-1-sulfonic acid and naphthalene-2-sulfonic acid into the corresponding hydroxylated compounds

Biotechnology Letters 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 C16H12O, Related Products of pyridine-derivatives.

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

Zhu, Heping published the artcileDiscovery of novel 2-aryl-3-sulfonamido-pyridines (HoAns) as microtubule polymerization inhibitors with potent antitumor activities, Related Products of pyridine-derivatives, the publication is European Journal of Medicinal Chemistry (2021), 113117, database is CAplus and MEDLINE.

In this study, a series of novel 2-aryl-3-sulfonamido-pyridines had been designed, synthesized, and evaluated for their antiproliferative activities in vitro and in vivo. Among them, compound I exhibited the most potent activity with IC₅₀ values ranging from 0.170 to 1.193μM in a panel of cancer cell lines. Mechanistic studies indicated that compound I bound to the colchicine site of β-tubulin, resulting in colony formation inhibition, G2/M phase cell cycle arrest, cell apoptosis as well as increased the generation of ROS in both RKO and SW620 cells. In addition, compound I showed potent anti-vascular activity in vitro. Furthermore, compound I also exhibited outstanding antitumor activity in SW620 xenograft tumor models without observable toxic effects, which was more potent than that of ABT-751. In conclusion, these findings suggest that compound I may be a promising microtubule destabilizing agent and deserves for further development in cancer therapy.

European 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 C9H7F3O3, Related Products of pyridine-derivatives.

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

Wu, Jing-wei published the artcileSynthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout, Formula: C5H5BrN2, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(3), 383-388, database is CAplus and MEDLINE.

Bromonaphthylmethyltriazolyl thioether lesinurad analogs and bioisosteres such as I were prepared as inhibitors of uric acid transporter 1 (URAT1) for potential use in treating hyperuricemia and gout. I inhibited URAT1 with an IC₅₀ value of 32 nM, 225-fold lower than lesinurad. The pharmacophore for the lesinurad analogs was determined using a 3D-QSAR pharmacophore model; the hypothesis was validated by three methods (cost anal., Fisher’s randomization and leave-one-out).

Bioorganic & Medicinal Chemistry Letters 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 C12H10FeO4, Formula: C5H5BrN2.

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

Zhang, Yu published the artcileA new tetraphosphine and its application in Pd-catalyzed Suzuki cross-coupling reaction, Recommanded Product: 5-Nitro-2-phenylpyridine, the publication is Youji Huaxue (2012), 32(4), 790-793, database is CAplus.

A new tetraphosphine, N,N,N’,N’-tetra(diphenylphosphinomethyl)-cyclohexane-1,2-diamine has been designed and synthesized from the com. available cyclohexane-1,2-diamine as starting material. This tetraphosphine in combination with [Pd(η³-C₃H₅)Cl]₂ is a very efficient catalyst for Suzuki cross-coupling reaction. Various aryl and heteroaryl chlorides or bromides could be successfully transformed to the desired products in up to 99% yield with 0.1 mol% catalyst loading.

Youji Huaxue 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 C7H7ClN2S, Recommanded Product: 5-Nitro-2-phenylpyridine.

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

Xia, Peng-Ju published the artcilePhotocatalytic, Phosphoranyl Radical-Mediated N-O Cleavage of Strained Cycloketone Oximes, Product Details of C5H6BNO2, the publication is Organic Letters (2019), 21(8), 2658-2662, database is CAplus and MEDLINE.

In the presence of the iridium photocatalyst [Ir[dF(CF₃)ppy]₂(dtbbpy)]PF₆, four-membered cyclic ketoximes such as cyclobutanone oxime underwent ring opening and addition reactions with aryl alkenes such as 1,1-diphenylethylene or with α-trifluoromethylstyrenes such as PhC(CF₃):CH₂ mediated by Ph₃P (via its photogenerated phosphoranyl radical cation) under blue LED light to yield 6-arylhexanenitriles such as Ph₂CH(CH₂)₄CN or (aryl)(difluoromethylene)hexanenitriles such as F₂C:CPh(CH₂)₄CN.

Organic Letters 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 C7H8BrClFN, Product Details of C5H6BNO2.

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

Zeng, Kui published the artcileAnomeric Stereoauxiliary Cleavage of the C-N Bond of D-Glucosamine for the Preparation of Imidazo[1,5-a]pyridines, Category: pyridine-derivatives, the publication is Chemistry – A European Journal (2022), 28(29), e202200648, database is CAplus and MEDLINE.

An anomeric stereoauxiliary approach for the synthesis of a wide range of imidazo[1,5-a]pyridines I (R¹ = Me, 2-methylphenyl, pyridin-2-yl, etc.; R² = 4-methoxyphenyl, naphthalen-1-yl, thiophen-2-yl, etc.) after cleaving the C-N bond of D-glucosamine (α-2° amine) from biobased resources was reported . This new approach expands the scope of readily accessible imidazo[1,5-a]pyridines I relative to existing state-of-the-art methods. A key strategic advantage of this approach is that the α-anomer of D-glucosamine enables C-N bond cleavage via a seven-membered ring transition state. By using this novel method, a series of imidazo[1,5-a]pyridine derivatives (>80 examples) was synthesized from 2-acylpyridines (including para-dipyridine ketone) and aldehydes (including para-dialdehyde) R²CHO. Imidazo[1,5-a]pyridine I derivatives containing diverse important deuterated C(sp²)-H and C(sp³)-H bonds were also efficiently achieved.

Chemistry – A European Journal 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 C15H10O2, Category: pyridine-derivatives.

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

Yang, Yu-Ming published the artcileSilver-Mediated Trifluoromethoxylation of (Hetero)aryldiazonium Tetrafluoroborates, HPLC of Formula: 39856-58-1, the publication is Organic Letters (2019), 21(19), 8003-8007, database is CAplus and MEDLINE.

Here we report a silver-mediated trifluoromethoxylation of (hetero)aryldiazonium tetrafluoroborates by converting an aromatic amino group into an OCF₃ group. This method, which can be considered to be a trifluoromethoxylation variation of the classic Sandmeyer-type reaction, uses readily available aryl and heteroaromatic amines as starting materials and AgOCF₃ as trifluoromethoxylating reagents. The broad substrate scope and simple, mild reaction condition made this transformation a valuable method in constructing aryl-OCF₃ bonds.

Organic Letters 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 C11H21BF4N2O2, HPLC of Formula: 39856-58-1.

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

Fu, Shibo published the artcileγ-H2AX kinetics as a novel approach to high content screening for small molecule radiosensitizers, Synthetic Route of 2215-33-0, the publication is PLoS One (2012), 7(6), e38465, database is CAplus and MEDLINE.

Background: Persistence of γ-H2AX after ionizing radiation (IR) or drug therapy is a robust reporter of unrepaired DNA double strand breaks in treated cells. Methods: DU-145 prostate cancer cells were treated with a chem. library ±IR and assayed for persistence of γ-H2AX using an automated 96-well immunocytochem. assay at 4 h after treatment. Hits that resulted in persistence of γ-H2AX foci were tested for effects on cell survival. The mol. targets of hits were validated by mol., genetic and biochem. assays and in vivo activity was tested in a validated Drosophila cancer model. Results: We identified 2 compounds, MS0019266 and MS0017509, which markedly increased persistence of γ-H2AX, apoptosis and radiosensitization in DU-145 cells. Chem. evaluation demonstrated that both compounds exhibited structurally similar and biochem. assays confirmed that these compounds inhibit ribonucleotide reductase. DNA microarray anal. and immunoblotting demonstrates that MS0019266 significantly decreased polo-like kinase 1 gene and protein expression. MS0019266 demonstrated in vivo antitumor activity without significant whole organism toxicity. Conclusions: MS0019266 and MS0017509 are promising compounds that may be candidates for further development as radiosensitizing compounds as inhibitors of ribonucleotide reductase.

PLoS One 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

Baba, Daisuke published the artcileElectrolytic partial fluorination of organic compounds. Part 62. Highly diastereoselective anodic fluorination of chiral 1,3-oxathiolan-5-ones derived from camphorsulfonamides, Quality Control of 107263-95-6, the publication is Journal of Fluorine Chemistry (2003), 121(1), 93-96, database is CAplus.

Anodic fluorination of chiral 1,3-oxathiolan-5-ones, derived from camphorsulfonamide and thioglycolic acid, was carried out under various conditions. When dimethoxyethane (DME) containing Et₄NF·4HF was used, the corresponding monofluorinated products were obtained in good yield as a single diastereomer. Chem. fluorination was also attempted using N-fluoropyridinium salts; however, fluorination did not proceed at all. The anodic fluorination of (+)-(1R,2R,4R)-7,7-dimethyl-N,N-bis(1-methylethyl)-5′-oxo-spiro[bicyclo[2.2.1]heptane-2,2′-[1,3]oxathiolane]-1-methanesulfonamide gave (+)-(1R,2R,4R,4′S)-4′-Fluoro-7,7-dimethyl-N,N-bis(1-methylethyl)-5′-oxo-spiro[bicyclo[2.2.1]heptane-2,2′-[1,3]oxathiolane]-1-methanesulfonamide (I). Crystal and mol. structures of I were reported.

Journal of Fluorine Chemistry published new progress about 107263-95-6. 107263-95-6 belongs to pyridine-derivatives, auxiliary class Fluorination reagent, name is 1-Fluoropyridiniumtriflate, and the molecular formula is C6H5F4NO3S, Quality Control of 107263-95-6.

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

Jahed, Zeinab published the artcileNanocrown electrodes for parallel and robust intracellular recording of cardiomyocytes, Recommanded Product: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Nature Communications (2022), 13(1), 2253, database is CAplus and MEDLINE.

Drug-induced cardiotoxicity arises primarily when a compound alters the electrophysiol. properties of cardiomyocytes. Features of intracellular action potentials (iAPs) are powerful biomarkers that predict proarrhythmic risks. In the last decade, a number of vertical nanoelectrodes have been demonstrated to achieve parallel and minimally-invasive iAP recordings. However, the large variability in success rate and signal strength have hindered nanoelectrodes from being broadly adopted for proarrhythmia drug assessment. In this work, we develop vertically-aligned nanocrown electrodes that are mech. robust and achieve > 99% success rates in obtaining intracellular access through electroporation. We validate the accuracy of nanocrown electrode recordings by simultaneous patch clamp recording from the same cell. Finally, we demonstrate that nanocrown electrodes enable prolonged iAP recording for continual monitoring of the same cells upon the sequential addition of four incremental drug doses. Our technol. development provides an advancement towards establishing an iAP screening assay for preclin. evaluation of drug-induced arrhythmogenicity.

Nature Communications 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