Month: December 2022

Naito, Yasuyuki published the artcileConstructing vascularized hepatic tissue by cell-assembled viscous tissue sedimentation method and its application for vascular toxicity assessment, Safety of Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Acta Biomaterialia (2022), 275-288, database is CAplus and MEDLINE.

In vitro Construction of the liver sinusoidal structure using artificial tissue is an important but worthwhile challenge, particularly for assessing the risk of diseases such as sinusoidal obstruction syndrome (SOS). Current models are unsuitable for evaluating the toxicity because of lacking sinusoidal capillary. In this study, we developed a vascularized hepatic tissue (VHT) using a unique tissue engineering technique, the cell assembled viscous tissue by sedimentation (CAViTs) method. The “viscous bodies” created using the CAViTs method exhibited significant self-assembly within 6 h after seeding, promoting cell-cell interaction. The level of albumin secreted by the VHT was four times higher than that of 2D-coculture and maintained for 1 mo. The gene expression pattern of the VHT was closer to that of total human liver, compared with the 2D system. Quant. evaluations of the vascular structure of VHT treated with two typical SOS-inducing compounds, monocrotaline and retrorsine, revealed higher sensitivity (IC50 = 40.35μM), 19.92 times higher than the cell-viability assay. Thus, VHT represents an innovative in vitro model that mimics the vessel network structure and could become a useful tool for the early screening of compounds associated with a risk of vascular toxicity. Mimicking sinusoidal structures in in vitro liver model is important to consider from the perspective of predicting hepatotoxicity such like sinusoidal obstruction syndrome (SOS). However, it was difficult to reconstruct the vascular structure within the hepatocyte-rich environment. In this study, we constructed a vascularized hepatic tissue in a high-throughput manner by a unique method using collagen and heparin, and evaluated its applicability to toxicity assessment. Vessel morphol. anal. of the model treated by monocrotaline, which is a well-known SOS-inducing compound, could predict the toxicity with higher sensitivity. To the best of our knowledge, this is the first report to provide vascularized hepatic tissues using sinusoidal endothelial cells at least for demonstrating applicability to the evaluation of SOS induction risk.

Acta Biomaterialia 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, 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

Owa, Takashi published the artcileSynthesis and biological evaluation of N-(7-indolyl)-3-pyridinesulfonamide derivatives as potent antitumor agents, Formula: C5H5NO3S, the publication is Bioorganic & Medicinal Chemistry Letters (2002), 12(16), 2097-2100, database is CAplus and MEDLINE.

The synthesis and antitumor activity of E7070 analogs containing a 3-pyridinesulfonamide moiety is reported. E7070 was selected from our sulfonamide-based compound collections, currently undergoing Phase II clin. trials because of its tolerable toxicity profile and some antitumor responses in the Phase I setting. Of the analogs examined, ER-35745 (I), a 6-amino-3-pyridinesulfonamide derivative, demonstrated significant oral efficacy against the HCT116 human colon carcinoma xenograft in nude mice.

Bioorganic & Medicinal Chemistry 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 C5H5NO3S, Formula: C5H5NO3S.

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

Kaburaki, Soyoko published the artcileHepatic drug metabolism in older people with body composition changes., Related Products of pyridine-derivatives, the publication is Geriatrics & gerontology international (2022), 22(5), 449-454, database is MEDLINE.

AIM: Dosage adjustment is essential in older individuals because they are prone to experience a decline in liver function and changes in body composition. However, quantitative tests or equations for evaluating the activity of hepatic drug metabolism have not yet been clearly established. We examined hepatic drug metabolism activities in older individuals, focusing on changes in body composition parameters. METHODS: Lansoprazole and nifedipine, substrates of the metabolic enzymes cytochrome P450 (CYP) 2C19 and 3A4, respectively, were selected to study hepatic drug metabolism. Residual samples from blood test for older patients were evaluated to determine drug metabolism. The body composition of relevant patients was determined by analyzing characteristic parameters of skeletal muscle mass index (SMI), handgrip strength (HGS) and hepatic steatosis index (HSI). The differences in hepatic drug metabolism were studied statistically among categories in terms of the cut-off value of these parameters. RESULTS: Older male patients receiving lansoprazole and nifedipine in the low SMI (<7.0 kg/m² ) category showed an 85-90% reduction in respective CYP2C19 and CYP3A4 metabolic activities compared with the normal SMI category. For the female patients, CYP2C19 and CYP3A4 metabolic activities showed no significant correlation with SMI and HGS. Fatty liver disease (HSI ≥36) was found to reduce CYP2C19 metabolic activity particularly in older female patients. CONCLUSIONS: Low CYP2C19 metabolic activity was statistically correlated with low SMI in male patients and high HSI in female patients, whereas low CYP3A4 metabolic activity was statistically correlated with low HGS in male patients. Geriatr Gerontol Int 2022; 22: 449-454.

Geriatrics & gerontology international 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, Related Products of pyridine-derivatives.

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

Takahashi, Kazunobu published the artcileDetermination of release rate of pyridine-triphenylborane (PTPB) from copper-free antifouling paints, COA of Formula: C23H20BN, the publication is Shikizai Kyokaishi (2005), 78(2), 50-57, database is CAplus.

Pyridine-triphenylborane (PTPB) is one of the alternative tin-free antifoulants in marine antifouling paints and was used widely in com. copper-free self-polishing antifouling paints in Japan. Anal. method for determination of PTPB at low ppb level in seawater was developed by HPLC with UV detection at 220 nm after pre-concentration with C18 solid-phase extraction (SPE). PTPB leached from an antifouling paint film was extracted from artificial seawater using a C18 solid-phase extraction (SPE) cartridge, and eluted with acetonitrile/pyridine (99:1). The recoveries of PTPB (25 μg/1 and 50 μg/l) spiked into artificial seawater were 96% and 97%, resp. The limit of determination of PTPB using 100 mL of artificial seawater was 0.5 μg/l for this anal. method. The HPLC-UV using SPE was applied onto measurement of the release rate (μg/cm²/day) of PTPB from copper-free antifouling paints containing PTPB according to both ISO 15181-1 and 15181-2.

Shikizai Kyokaishi published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C6H12N2O, COA of Formula: C23H20BN.

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

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