Day: December 5, 2022

Drumm, Bernard T. published the artcileCa²⁺ signaling in interstitial cells of Cajal contributes to generation and maintenance of tone in mouse and monkey lower oesophageal sphincters, Related Products of pyridine-derivatives, the publication is Journal of Physiology (Oxford, United Kingdom) (2022), 600(11), 2613-2636, database is CAplus and MEDLINE.

The lower oesophageal sphincter (LES) generates tone and prevents reflux of gastric contents. LES smooth muscle cells (SMCs) are relatively depolarised, facilitating activation of Ca_v1.2 channels to sustain contractile tone. We hypothesised that i.m. interstitial cells of Cajal (ICC-IM), through activation of Ca²⁺-activated Cl^– channels (ANO1), set membrane potentials of SMCs favorable for activation of Ca_v1.2 channels. In some gastrointestinal muscles, ANO1 channels in ICC-IM are activated by Ca²⁺ transients, but no studies have examined Ca²⁺ dynamics in ICC-IM within the LES. Immunohistochem. and qPCR were used to determine expression of key proteins and genes in ICC-IM and SMCs. These studies revealed that Ano1 and its gene product, ANO1, are expressed in c-Kit ⁺cells (ICC-IM) in mouse and monkey LES clasp muscles. Ca²⁺ signalling was imaged in situ, using mice expressing GCaMP6f specifically in ICC (Kit-KI-GCaMP6f). ICC-IM exhibited spontaneous Ca²⁺ transients from multiple firing sites. Ca²⁺ transients were abolished by cyclopiazonic acid or caffeine but were unaffected by tetracaine or nifedipine. Maintenance of Ca²⁺ transients depended on Ca²⁺ influx and store reloading, as Ca²⁺ transient frequency was reduced in Ca²⁺ free solution or by Orai antagonist. Spontaneous tone of LES muscles from mouse and monkey was reduced ∼80% either by Ani9, an ANO1 antagonist or by the Ca_v1.2 channel antagonist nifedipine. Membrane hyperpolarisation occurred in the presence of Ani9. These data suggest that intracellular Ca²⁺ activates ANO1 channels in ICC-IM in the LES. Coupling of ICC-IM to SMCs drives depolarisation, activation of Ca_v1.2 channels, Ca²⁺ entry and contractile tone.

Journal of Physiology (Oxford, United Kingdom) 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

Liu, Shan-Shan published the artcileSulfonic Groups Lined along Channels of Metal-Organic Frameworks (MOFs) for Super-Proton Conductor, Computed Properties of 636-73-7, the publication is Inorganic Chemistry (2020), 59(1), 396-402, database is CAplus and MEDLINE.

Designing high-performance proton-conducting metal-organic frameworks simultaneously having highly hydrothermal stability and a high-d. proton carrier remains a great challenge. Fe-MIL-88B is a classic metal-organic framework (MOF) with a large-size one-dimensional (1D) channel lined with a high-d. uncoordinated metal atom for postfunctionalization; however this MOF cannot act as a proton conductor due to the weak hydrothermal stability. Here, we prepared an ultrastable isostructure Cr-MIL-88B, which is subsequently functionalized by anchoring 3-pyridinesulfonic acid and 2-(4-pyridyl) ethanesulfonic acid on the naked Cr atoms exposed on the surface of the host-framework, producing two new MOFs, i.e. Cr-MIL-88B-pyridine sulfonic acid (abbreviated as Cr-MIL-88B-PSA) and Cr-MIL-88B-pyridine ethanesulfonic acid (abbreviated as Cr-MIL-88B-PESA). Thus, Cr atoms on the host framework were modified by functional sulfonic groups, which stick out toward the center of the channel forming ordered high-d. sulfonic groups as proton donors along the open channel and achieving the highest proton conductivity of 4.50 × 10^-2 S cm^-1 for Cr-MIL-88B-PESA and 1.58 × 10^-1 S cm^-1 for Cr-MIL-88B-PSA, surpassing that of the Nafion membrane.

Inorganic 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, Computed Properties of 636-73-7.

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

Lee, Jongkook published the artcileSynthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors, Recommanded Product: 2-Pyridinylboronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(12), 4044-4048, database is CAplus and MEDLINE.

A series of hydroxybenzoxazole derivatives, e.g., I [R² = H, Cl, MeNH, MeCONH, R³ = H, MeCO, Me(OH)CH, 3-pyrazolyl, etc., R⁴ = H, 2-pyridinyl, 4-MeOC₆H₄, Me₂CHNH], was synthesized, and their c-Met kinase inhibitory activity was evaluated. Described herein is a potent c-Met inhibitor by structural modification of the parent benzoxazole scaffold, with particular focus on the hydroxyl substituent of the benzoxazole moiety.

Bioorganic & Medicinal Chemistry 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 C5H6BNO2, Recommanded Product: 2-Pyridinylboronic acid.

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

Liu, Chun published the artcileA General and Highly Efficient Method for the Construction of Aryl-Substituted N-Heteroarenes, Application In Synthesis of 89076-64-2, the publication is European Journal of Organic Chemistry (2010), 5548-5551, S5548/1-S5548/23, database is CAplus.

A general, simple and highly efficient method for the synthesis of heteroarylbenzenes has been developed via Pd(OAc)₂-catalyzed ligand-free and aerobic Suzuki coupling reaction of N-heteroaryl halides with arylboronic acids and the reaction is strongly dependent on the mol. structure of solvent.

European Journal of Organic Chemistry 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, Application In Synthesis of 89076-64-2.

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

Lawson, Marie published the artcileAn efficient coupling of N-tosylhydrazones with 2-halopyridines: synthesis of 2-α-styrylpyridines endowed with antitumor activity, SDS of cas: 39856-58-1, the publication is Organic & Biomolecular Chemistry (2013), 11(22), 3664-3673, database is CAplus and MEDLINE.

The synthesis of 2-α-styrylpyridines has been carried out by using the coupling of polyoxygenated N-tosylhydrazones with various 2-halopyridines. We demonstrated that the use of a catalytic amount of PdCl₂(MeCN)₂ in combination with a bidentate ferrocene DPPF or a monodentate alkyl phosphine ^tBu₂MeP-HBF₄ constitutes an efficient protocol for this coupling, providing 2-α-styrylpyridines in satisfactory to good yields. Among evaluated, compound I was found to exhibit excellent antiproliferative and antimitotic activities comparable to that of the reference compound isoCA-4.

Organic & Biomolecular 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, SDS of cas: 39856-58-1.

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

Kato, Tetsuzo published the artcileSynthesis of methylpyridine derivatives. X. The Skraup reaction of 4-aminomethylpyridine 1-oxides, Formula: C6H8N2, the publication is Pharmaceutical Bulletin (1956), 178-81, database is CAplus and MEDLINE.

To prepare the rare 1,6-naphthyridine 6-oxide (I) derivatives, the Skraup reaction was applied to the easily available 4-amino-2,6-lutidine 1-oxide (II), 4-amino-3-picoline 1-oxide (III), 4-amino-2-picoline 1-oxide (IV), and 4-aminopyridine 1-oxide (V). Adding 2.75 g. concentrated H₂SO₄ dropwise to 1.38 g. II, 1.38 g. As₂O₅, and 3.68 g. glycerol, heating the mixture 3 hrs. in an oil bath at 155°, cooling, adding 50 cc. ice H₂O, making alk. with Na₂CO₃, and extracting with 200 cc. CHCl₃ yielded from the decolorized CHCl₃ extract 0.15 g. 5,7-di-Me derivative (VI) of I, white needles, m. 127-32° (from C₆H₆ or Me₂CO); picrate, yellow needles, m. 194-6° (from MeOH). Similar treatment gave (g. starting material, g. derivative of I formed, nature of crystals, m.p., and m.p. of picrate given): 3 g. III, 0.2 g. 8-Me (VII), white needles, 187-8.5° (from Me₂CO), 170-2°; 12.4 g. IV, 0.85 g. 7(or 5)-Me (VIII), white needles, 158-9° (from C₆H₆, 216-19° (decomposition); 1.1 g. V, 0.09 g. I, pale yellow needles, 151° (from C₆H₆ or Me₂CO), 185-6°. IV, m. 122-8° (picrate, m. 180°; HCl salt, m. 192°), and V, m. 229° (picrate, m. 201.5-2.0°), were prepared according to K. and H. (preceding abstract) from 4-nitro-2-picoline 1-oxide and 4-nitro-pyridine 1-oxide by catalytic reduction with 50% Pd-C in H₂O in 92% and 88% yield, resp. The yields of all 4 derivatives of I were only 5-9%. Ultraviolet absorption curves were given for I-VIII.

Pharmaceutical Bulletin 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, Formula: C6H8N2.

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

Hallinan, E. A. published the artcile2,4-Disubstituted oxazoles and thiazoles as latent pharmacophores for diacylhydrazine of SC-51089, a potent PGE₂ antagonist, Recommanded Product: 4-Amino-2-picoline, the publication is Bioorganic & Medicinal Chemistry (2001), 9(1), 1-6, database is CAplus and MEDLINE.

8-Chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-[1-oxo-3-(4-pyridinyl)propyl]hydrazide, monohydrochloride (SC-51089) is a functional PGE₂ antagonist selective for the EP₁ receptor subtype with antinociceptive activity. Analogs of SC-51089, in which the diacylhydrazine moiety has been replaced with 2,4-disubstituted-oxazoles and-thiazoles, are described. The analgesic activity seen among the oxazoles does not correlate with its PGE₂ antagonism.

Bioorganic & Medicinal Chemistry 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, Recommanded Product: 4-Amino-2-picoline.

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

Qu, Bo published the artcileChelation controlled reductive amination of cyclic ketones to trans-4-methoxycyclohexylamines: 9-BBN reduction mediated with FeCl₃, Application of 2-Bromopyridin-3-amine, the publication is Tetrahedron Letters (2012), 53(15), 1982-1986, database is CAplus.

A novel trans-diastereoselective reductive amination of 4-substituted cyclohexanones is described using 9-BBN as reducing agent in the presence of FeCl₃. The method permits efficient synthesis of structurally diverse 4-trans-alkoxycyclohexylamines.

Tetrahedron 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 C5H5BrN2, Application of 2-Bromopyridin-3-amine.

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

Bell, Meghan M. published the artcileGlypican-3-targeted alpha particle therapy for hepatocellular carcinoma, Formula: C26H36N4O8, the publication is Molecules (2021), 26(1), 4, database is CAplus and MEDLINE.

Glypican-3 (GPC3) is expressed in 75% of hepatocellular carcinoma (HCC), but not normal liver, making it a promising HCC therapeutic target. GC33 is a full-length humanized monoclonal IgG1 specific to GPC3 that can localize to HCC in vivo. GC33 alone failed to demonstrate therapeutic efficacy when evaluated in patients with HCC; however, we posit that cytotoxic functionalization of the antibody with therapeutic radionuclides, may be warranted. Alpha particles, which are emitted by radioisotopes such as Actinium-225 (Ac-225) exhibit high linear energy transfer and short pathlength that, when targeted to tumors, can effectively kill cancer and limit bystander cytotoxicity. Macropa, an 18-member heterocyclic crown ether, can stably chelate Ac-225 at room temperature Here, we synthesized and evaluated the efficacy of [225Ac]Ac-Macropa-GC33 in mice engrafted with the GPC3-expressing human liver cancer cell line HepG2. Following a pilot dose-finding study, mice (n = 10 per group) were treated with (1) PBS, (2) mass-equivalent unmodified GC33, (3) 18.5 kBq [225Ac]Ac-Macropa-IgG1 (isotype control), (4) 9.25 kBq [225Ac]Ac-Macropa-GC33, and (5) 18.5 kBq [225Ac]Ac-Macropa-GC33. While significant toxicity was observed in all groups receiving radioconjugates, the 9.25 kBq [225Ac]Ac-Macropa-GC33 group demonstrated a modest survival advantage compared to PBS (p = 0.0012) and 18.5 kBq [225Ac]Ac-IgG1 (p = 0.0412). Hematol. anal. demonstrated a marked, rapid reduction in white blood cells in all radioconjugate-treated groups compared to the PBS and unmodified GC33 control groups. Our studies highlight a significant disadvantage of using directly-labeled biomols. with long blood circulation times for TAT. Strategies to mitigate such treatment toxicity include dose fractionation, pretargeting, and using smaller targeting ligands.

Molecules published new progress about 1128304-86-8. 1128304-86-8 belongs to pyridine-derivatives, auxiliary class Pyridines, name is 6,6′-((1,4,10,13-Tetraoxa-7,16-diazacyclooctadecane-7,16-diyl)bis(methylene))dipicolinic acid, and the molecular formula is C26H36N4O8, Formula: C26H36N4O8.

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

Garai, Rabindranath published the artcileTriple Passivation Approach to Laminate Perovskite Layers for Augmented UV and Ambient Stable Photovoltaics, Recommanded Product: Phenyl(pyridin-2-yl)methanone, the publication is ACS Applied Energy Materials (2022), 5(3), 3392-3400, database is CAplus.

The instability of the perovskite solar cells (PSCs) toward UV irradiation and moisture is a limiting factor in terms of commercialization even after achieving excellent power conversion efficiencies (PCEs). Herein, an advanced triple passivation technique has been strategically designed and demonstrated utilizing UV-absorbing 2-benzoylpyridine (BP) mols. as a passivation additive to laminate perovskites and improve PSC stability. Double layers of BP were coated on both sides of the perovskite layer, and the mol. was also incorporated into the precursor solution This strategy significantly improved the perovskite crystallinity and film quality, lowered the recombination, and enhanced the carrier transport in the PSC. The triple-passivated device exhibited a high PCE of 20.46% with almost negligible hysteresis. Further, passivated large-area (2.5 cm²) devices were also fabricated that demonstrated a PCE of 18.61%. Moreover, the triple passivation approach exhibited impressive UV and ambient stability because it can effectively shield the perovskite layer from UV illumination and moisture.

ACS Applied Energy Materials 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, Recommanded Product: Phenyl(pyridin-2-yl)methanone.

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