Category: pyridine-derivatives

Miura, Hiroki published the artcileRuthenium-Catalyzed Intermolecular Hydroacylation of Internal Alkynes: The Use of Ceria-Supported Catalyst Facilitates the Catalyst Recycling, HPLC of Formula: 71255-09-9, the main research area is conjugated enone preparation; ceria supported ruthenium hydroacylation alkyne aldehyde.

Intermol. hydroacylation of internal alkynes by aromatic aldehydes, catalyzed by Ru/CeO2 or [RuCl2(p-cymene)]2 in the presence of sodium formate and Xantphos, gave conjugated enones. E.g., in presence of Ru/CeO2, hydroacylation of PhCCPh by PhCHO gave 52% enone I (64:36 E/Z). The solid Ru/CeO2 continued to show catalytic activity and gave enones without significant decreases in yields for at least three times.

Chemistry – A European Journal published new progress about Alkynes, internal Role: RCT (Reactant), RACT (Reactant or Reagent). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, HPLC of Formula: 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ramil, Carlo P. published the artcileSequence-Specific 2-Cyanobenzothiazole Ligation, HPLC of Formula: 133627-45-9, the main research area is cyanobenzothiazole ligation protein labeling.

The use of small, natural chem. reporters in conjunction with catalyst-free bioorthogonal reactions will greatly streamline protein labeling in a cellular environment with min. perturbation to their function. Here we report the discovery of a 2-cyanobenzothiazole (CBT)-reactive peptide tag, CX10R7, from a cysteine-encoded peptide phage library using the phage-assisted interrogation of reactivity method. Fusion of CX10R7 with a protein of interest allows site-specific labeling of the protein with CBT both in vitro and on the surface of E. coli cells. Mutagenesis studies indicated that the reactivity and specificity of CX10R7 are attributed to the sequence environment, in which the residues surrounding cysteine help to stabilize the ligation product.

Journal of the American Chemical Society published new progress about Aromatic nitriles Role: RCT (Reactant), RACT (Reactant or Reagent). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, HPLC of Formula: 133627-45-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Perez-Pineiro, Rolando published the artcileSynthesis of sulfur-containing aryl and heteroaryl vinyls via Suzuki-Miyaura cross-coupling for the preparation of SERS-active polymers, Product Details of C6H8BNO2S, the main research area is sulfur aryl heteroaryl viny Suzuki coupling.

The preparation of sulfur-containing aryl and heteroaryl vinyl co-monomers via Suzuki-Miyaura cross-coupling between the corresponding mercaptomethyl arylboronates and in situ-generated vinyl bromides is described. Surface-enhanced Raman scattering (SERS) studies of the target compounds on gold nanoparticles confirmed their potential as spectroscopic tags in the fabrication of SERS-encoded polymers for combinatorial screening and biomedical diagnostics.

Tetrahedron Letters published new progress about Aryl alkenes Role: SPN (Synthetic Preparation), PREP (Preparation). 321438-86-2 belongs to class pyridine-derivatives, name is 6-(Methylthio)pyridin-3-ylboronic acid, and the molecular formula is C6H8BNO2S, Product Details of C6H8BNO2S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Swahn, Britt-Marie published the artcileDesign and Synthesis of β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors with in Vivo Brain Reduction of β-Amyloid Peptides, SDS of cas: 917471-30-8, the main research area is aminoisoindole BACE1 inhibitor brain reduction beta amyloid peptide.

The evaluation of a series of aminoisoindoles as β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors and the discovery of a clin. candidate drug for Alzheimer’s disease, (S)-32 (I, AZD3839), are described. The improvement in permeability properties by the introduction of fluorine adjacent to the amidine moiety, resulting in in vivo brain reduction of Aβ40, is discussed. Due to the basic nature of these compounds, they displayed affinity for the human ether-a-go-go related gene (hERG) ion channel. Different ways to reduce hERG inhibition and increase hERG margins for this series are described, culminating in (S)-16 (II) and (R)-41 (III) showing large in vitro margins with BACE1 cell IC50 values of 8.6 and 0.16 nM, resp., and hERG IC50 values of 16 and 2.8 μM, resp. Several compounds were advanced into pharmacodynamic studies and demonstrated significant reduction of β-amyloid peptides in mouse brain following oral dosing.

Journal of Medicinal Chemistry published new progress about Absolute configuration (enantiomer preference for enzyme binding). 917471-30-8 belongs to class pyridine-derivatives, name is (5-(Prop-1-yn-1-yl)pyridin-3-yl)boronic acid, and the molecular formula is C8H8BNO2, SDS of cas: 917471-30-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Huiping published the artcileSynthesis of 2-cyanoacrylates containing pyridinyl moiety under ultrasound irradiation, COA of Formula: C6H7ClN2, the main research area is pyridinylaminocyanoacrylate preparation antitumor; cyanoacrylate pyridinylamino preparation antitumor; methylthiocyanoacrylate pyridinamine substitution ultrasound.

Reaction of NCCH2CO2Et with CS2 and Me2SO4 in the presence of NaOMe in anhydrous MeOH yields 2-cyano-3,3-bis(methylthio)acrylate. Further nucleophilic substitution with 3-amino-2-chloro-4-methylpyridine under ultrasonic irradiation afforded 3-[(2-chloro-4-methylpyridin-3-yl)amino]-2-cyano-3-methylthioacrylate as key intermediate. The title compounds were then obtained through the reaction of the key intermediate with primary aliphatic amines under reflux. All new structures were verified by elemental anal., IR, 1H NMR and mass spectra. In the MTT test, the compounds were found to possess moderate antitumor activities against PC3 and A431 cells.

Journal of Heterocyclic Chemistry published new progress about Aliphatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, COA of Formula: C6H7ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Yaping published the artcileOne-Pot Double Benzylation of 2-Substituted Pyridines using Palladium-Catalyzed Decarboxylative Coupling of sp2 and sp3 Carbons, Application of 3-Methylpicolinic acid hydrochloride, the main research area is diarylmethane preparation; picolinic acid benzyl bromide decarboxylative double benzylation palladium silver.

An efficient and practical decarboxylative double benzylation method for various 2-picolinic acids has been established by using a bimetallic catalytic system of palladium(II) chloride (PdCl2) and silver(I) oxide (Ag2O), which offered a variety of diarylmethane derivatives e.g., I, with moderate to good yields.

Advanced Synthesis & Catalysis published new progress about Aralkyl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 123811-72-3 belongs to class pyridine-derivatives, name is 3-Methylpicolinic acid hydrochloride, and the molecular formula is C7H8ClNO2, Application of 3-Methylpicolinic acid hydrochloride.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

S’ari, Mark published the artcileLow dose scanning transmission electron microscopy of organic crystals by scanning moire fringes, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is STEM scanning moire fringes organic crystals; Bright field STEM; Dose-limited resolution; Low dose; Organic crystals; Scanning moiré fringes.

In the pharmaceutical industry, it is important to determine the effects of crystallization and processes, such as milling, on the generation of crystalline defects in formulated products. Conventional transmission electron microscopy and scanning transmission electron microscopy (STEM) can be used to obtain information on length scales unobtainable by other techniques, however, organic crystals are extremely susceptible to electron beam damage. This work demonstrates a bright field (BF) STEM method that can increase the information content per unit specimen damage by the use of scanning moire fringes (SMFs). SMF imaging essentially provides a magnification of the crystal lattice through the interference between closely aligned lattice fringes and a scanning lattice of similar spacing. The generation of SMFs is shown for three different organic crystals with varying electron beam sensitivity, theophylline, furosemide and felodipine. The electron fluence used to acquire the BF-STEM for the most sensitive material, felodipine was approx. 3.5 e-/Å2. After one addnl. scan of felodipine (total fluence of approx. 7.0 e-/Å2), the SMFs were no longer visible due to extensive damage caused to the crystal. Irregularity in the SMFs suggested the presence of defects in all the organic crystals. Further effort is required to improve the data anal. and interpretation of the resulting SMF images, allowing more information regarding the crystal structure and defects to be extracted

Micron published new progress about Crocidolite asbestos Role: ANT (Analyte), ANST (Analytical Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Charushin, Valery N. published the artcilePyrimidines. Part 93. Ring transformations of heterocycles. Part 28. Ring transformations of 5-nitropyrimidine via inverse Diels-Alder reactions, Safety of 4-(5-Nitropyridin-2-yl)morpholine, the main research area is nitropyrimidine inverse Diels Alder ketene; nitropyridine; pyrimidine nitro Diels Alder ketene; enamine Diels Alder nitropyrimidine.

5-Nitropyrimidine (I) underwent inverse Diels-Alder cycloaddition reactions with ketene acetals and enamines to give pyridine derivatives Thus, reaction of I with morpholinocyclohexene in EtOH at 70° for 2 h gave 80% pyridine II. 1H NMR studies showed the reaction involves a bicyclic intermediate.

Tetrahedron Letters published new progress about Acetals, ketene Role: RCT (Reactant), RACT (Reactant or Reagent). 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Safety of 4-(5-Nitropyridin-2-yl)morpholine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Choe, So-Hui published the artcileEffect of nifedipine, a calcium channel blocker, on the generation of nitric oxide and interleukin-1β by murine macrophages activated by lipopolysaccharide from Prevotella intermedia, Related Products of pyridine-derivatives, the main research area is calcium blockeron nitric oxide interleukin 1 beta lipopolysaccharide; Interleukin-1β; Lipopolysaccharide; Nifedipine; Nitric oxide; Periodontal disease.

The current study was undertaken to explore the influence of nifedipine on the generation of proinflammatory mediators by murine macrophages activated by lipopolysaccharide (LPS) prepared from Prevotella intermedia, a putative periodontal pathogen, and associated mechanisms of action as well. Real-time PCR and immunoblotting were conducted to quantify mRNA and protein expression, resp. NF-κB-dependent secreted embryonic alk. phosphatase (SEAP) levels were estimated by reporter assay. Nifedipine markedly suppressed the generation of iNOS-derived NO and IL-1β together with their mRNA expressions in murine macrophages activated by P. intermedia LPS. LPS-stimulated cells exposed to nifedipine notably increased the mRNA levels of Arg-1, Ym-1, FIZZ1, and TGF-β, which are typical markers for M2 macrophage polarization. Nifedipine induced HO-1 at both gene and protein levels in cells challenged with P. intermedia LPS, and the nifedipine-mediated inhibition of NO generation was significantly abrogated by adding SnPP, an HO-1 inhibitor. Nifedipine inhibited LPS-evoked generation of NO and IL-1β in a PPAR-γ-independent manner. Nifedipine is an inhibitor of P. intermedia LPS-evoked production of NO and IL-1β in murine macrophages and encourages macrophage polarization toward the M2 phenotype. Nifedipine possibly has potential to be used for host modulation of periodontal disease and is worth being further researched.

Naunyn-Schmiedeberg’s Archives of Pharmacology published new progress about Antigens, LyM-1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 21829-25-4 belongs to class pyridine-derivatives, 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:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Itsumi, Momoe published the artcileHigh-throughput screen identifies 5-HT receptor as a modulator of AR and a therapeutic target for prostate cancer, Name: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is antitumor AR modulator 5HT receptor therapeutic target prostate cancer; 5-hydroxytryptamine receptor; androgen receptor; high-throughput screen; prostate cancer; protein kinase A.

Background : Eradication of persistent androgen receptor (AR) activity in castration-resistant prostate cancer may be a promising strategy to overcome castration resistance. We aimed to identify novel compounds that inhibit AR activity and could be potential therapeutic agents for prostate cancer. Methods : A high-throughput screening system involving cell lines stably expressing AR protein and AR-responsive luciferase was employed for the 1260 compound library. Mol. and antitumor effects on candidate pathways that interacted with AR signaling were examined in prostate cancer cells expressing AR. Results : The high-throughput screening identified various potential compounds that interfered with AR signaling through known and novel pathways. Among them, a 5-hydroxytryptamine 5A (5-HT5A) receptor antagonist suppressed AR activity through protein kinase A signaling, which was confirmed by 5-HT5A receptor knockdown. Consistently, 5-HT5A receptor inhibitors showed cytotoxic effects toward prostate cancer cells. Conclusions : Taken together, this study identifies 5-HT5A receptor as a promising therapeutic target for prostate cancer via its interaction with AR signaling.

Prostate (Hoboken, NJ, United States) published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Name: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem