Category: pyridine-derivatives

Jiang, Min published the artcileA Facile Copper-Catalyzed One-Pot Domino Synthesis of 5,12-Dihydroindolo[2,1-b]quinazolines, Recommanded Product: 2-Bromopyridin-3-amine, the publication is Organic Letters (2012), 14(6), 1420-1423, database is CAplus and MEDLINE.

A domino synthesis of 5,12-dihydroindolo[2,1-b]quinazoline derivatives via copper-catalyzed Ullmann-type intermol. C-C and intramol. C-N couplings is reported. Good yields of various 5,12-dihydroindolo[2,1-b]quinazoline derivatives were obtained. Reaction scopes, limitations, and the reaction mechanism are discussed.

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 C5H5BrN2, Recommanded Product: 2-Bromopyridin-3-amine.

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

Sun, Maolin published the artcilePractical and rapid construction of 2-pyridyl ketone library in continuous flow, Synthetic Route of 91-02-1, the publication is Journal of Flow Chemistry (2021), 11(2), 91-98, database is CAplus.

Herein, a practical method for the rapid synthesis of 2-pyridyl ketone ArC(O)R [Ar = 2-pyridyl; R = Me, Ph, Bn, etc.] library in continuous flow was reported, in which the 2-lithiopyridine formed by Br/Li exchange reacts with com. available esters to obtain 2-pyridyl ketones ArC(O)R in a good yield at short reaction time. This protocol functions broadly on a variety of esters and had been applied to the synthesis of TGF-β type 1 receptor inhibitor LY580276 intermediate ArC(O)R [Ar = 6-methyl-2-pyridyl; R = (4-fluorophenyl)methyl] in an environmentally friendly method. It was rapid, reliable, and cost-efficient to afford diverse kinds of 2-pyridyl ketones ArC(O)R in the compound library.

Journal of Flow Chemistry 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 C19H36BNO2Si, Synthetic Route of 91-02-1.

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

Mu, Bing published the artcilePd-Catalyzed Tandem Cyclization via C-H Arylation and Acylation for the Construction of Polycyclic Scaffolds, Computed Properties of 1174626-28-8, the publication is Organic Letters (2016), 18(20), 5260-5263, database is CAplus and MEDLINE.

The first Pd-catalyzed tandem cyclization of imidazo[1,2-a]pyridines with 2-chlorobenzaldehydes through C-H arylation and acylation is presented for the efficient synthesis of novel 6H-benzo[b]imidazo[5,1,2-de]quinolizin-6-ones. The direct acylation reaction proceeded smoothly without the aid of directing groups and in the presence of air as a clean and free terminal oxidant.

Organic Letters published new progress about 1174626-28-8. 1174626-28-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine,Benzene,Ether, name is 2-Amino-6-benzyloxypyridine, and the molecular formula is C12H12N2O, Computed Properties of 1174626-28-8.

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

Gu, Xiaoke published the artcileDiscovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells, COA of Formula: C12H9NO, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(24), 127638, database is CAplus and MEDLINE.

P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a major obstacle to successful chemotherapy for leukemia. A series of thiosemicarbazone-containing compounds were synthesized. Biol. evaluation showed that the most active compound (E)-6-(2-(1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamido)-N-hydroxyhexanamide displayed potent anti-leukemia activity against P-gp overexpressing drug-resistant K562/A02 cells, with an IC₅₀ value of 0.44μM. Notably, compound (E)-6-(2-(1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamido)-N-hydroxyhexanamide exhibited a selective killing effect on K562/A02 cells by dose-dependently increasing the intracellular levels of reactive oxygen species (ROS), thus exerting a potential collateral sensitivity (CS)-promoting effect in vitro. Moreover, compound (E)-6-(2-(1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamido)-N-hydroxyhexanamide could inhibit HDAC1 and HDAC6, and induce the apoptosis of K562/A02 cells by increasing the expression of Bax, decreasing Bcl-2 protein level, and promoting the cleavage of caspase-3 and PARP, resp. Overall, (E)-6-(2-(1-(4-bromophenyl)ethylidene)hydrazine-1-carbothioamido)-N-hydroxyhexanamide may be a potential anti-cancer agent against drug-resistant myelogenous leukemia.

Bioorganic & Medicinal Chemistry Letters 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, COA of Formula: C12H9NO.

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

Zhang, Zixu published the artcilePhotocatalytic antifouling coating based on carbon nitride with dynamic acrylate boron fluorinated polymers, Product Details of C23H20BN, the publication is New Journal of Chemistry (2021), 45(2), 780-787, database is CAplus.

Based on the situation of marine biofouling and the ecol. crisis caused by toxic antifouling paints, a series of environmental carbon nitride (C₃N₄) nanocomposite films (CNPs) were prepared by incorporating C₃N₄ into a self-polishing acrylate boron fluorinated polymer (ABFP). The antifouling performance was evaluated by the diatom anti-attachment test, photocatalytic antibacterial measurements and a mussel settlement assay. The results showed that the optimal content of C₃N₄ to inhibit the adhesion of diatoms was 3-7 wt%, the antibacterial rate of Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli) reached 98.10% and 96.94% in the presence of 7 wt% C₃N₄ under irradiation with visible light for 90 min. In addition, the CNPs and ABFP showed an ability to expel mussels. As a synergistic effect, the self-renewable polymer surfaces could also strip the attached fouling organisms without light. The undifferentiated growth rates between the CNPs and blank proved the environmental properties of the prepared films. The COD values showed that the addition of C₃N₄ contributed to the eco-friendly properties of the CNPs.

New Journal of Chemistry 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 C7H11N, Product Details of C23H20BN.

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

Zhang, Li published the artcileRegioselective synthesis of polysubstituted N2-alkyl/aryl-1,2,3-triazoles via 4-bromo-5-iodo-1,2,3-triazole, Category: pyridine-derivatives, the publication is Synlett (2012), 23(7), 1052-1056, database is CAplus.

The regioselective N(2)-substitution of 4-bromo-5-iodo-1,2,3-triazole with alkyl/aryl halides in the presence of K₂CO₃ in DMF produced the desired 2-substituted 4-bromo-5-iodo-1,2,3-triazoles as major products in good to excellent regioselectivity. Subsequent chemoselective Suzuki-Miyaura cross-coupling of N(2)-substituted 4-bromo-5-iodo-1,2,3-triazoles provided polysubstituted 1,2,3-triazoles efficiently.

Synlett 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 C13H10N2S, Category: pyridine-derivatives.

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

Li, Shikai published the artcileInhibition of Sympathetic Activation by Delivering Calcium Channel Blockers from a 3D Printed Scaffold to Promote Bone Defect Repair, Related Products of pyridine-derivatives, the publication is Advanced Healthcare Materials (2022), 11(16), 2200785, database is CAplus and MEDLINE.

Enhancing osteogenesis by promoting neural network reconstruction and neuropeptide release is considered to be an attractive strategy for repairing of critical size bone defects. However, traumatic bone defects often activate the damaged sympathetic nervous system (SNS) in the defect area and release excessive catecholamine to hinder bone defect repair. Herein, a 3D printed scaffold loaded with the calcium channel blocker-nifedipine is proposed to reduce the concentration of catecholamine present in the bone defect region and to accelerate bone healing. To this end, nifedipine-loaded ethosome and laponite are added into a mixed solution containing sodium alginate, methacrylated gelatin, and bone mesenchymal stem cells (BMSCs) to prepare a cell-laden scaffold using 3D bioprinting. The released nifedipine is able to close the calcium channels of nerve cells, thereby blocking sympathetic activation and ultimately inhibiting the release of catecholamine by sympathetic nerve cells, which further promotes the osteogenic differentiation and migration of BMSCs, inhibits osteoclastogenesis in vitro, and effectively improves bone regeneration in a rat critical-size calvarial defect model. Therefore, the results suggest that sustained release of nifedipine from the scaffold can effectively block SNS activation, providing promising strategies for future treatment of bone defects.

Advanced Healthcare Materials 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

Yang, Biao published the artcileA conductive supramolecular hydrogel creates ideal endogenous niches to promote spinal cord injury repair, Product Details of C17H18N2O6, the publication is Bioactive Materials (2022), 103-119, database is CAplus and MEDLINE.

The current effective method for treatment of spinal cord injury (SCI) is to reconstruct the biol. microenvironment by filling the injured cavity area and increasing neuronal differentiation of neural stem cells (NSCs) to repair SCI. However, the method is characterized by several challenges including irregular wounds, and mech. and elec. mismatch of the material-tissue interface. In the current study, a unique and facile agarose/gelatin/polypyrrole (Aga/Gel/PPy, AGP3) hydrogel with similar conductivity and modulus as the spinal cord was developed by altering the concentration of Aga and PPy. The gelation occurred through non-covalent interactions, and the phys. crosslinked features made the AGP3 hydrogels injectable. In vitro cultures showed that AGP3 hydrogel exhibited excellent biocompatibility, and promoted differentiation of NSCs toward neurons whereas it inhibited over-proliferation of astrocytes. The in vivo implanted AGP3 hydrogel completely covered the tissue defects and reduced injured cavity areas. In vivo studies further showed that the AGP3 hydrogel provided a biocompatible microenvironment for promoting endogenous neurogenesis rather than glial fibrosis formation, resulting in significant functional recovery. RNA sequencing anal. further indicated that AGP3 hydrogel significantly modulated expression of neurogenesis-related genes through intracellular Ca2+ signaling cascades. Overall, this supramol. strategy produces AGP3 hydrogel that can be used as favorable biomaterials for SCI repair by filling the cavity and imitating the physiol. properties of the spinal cord.

Bioactive Materials 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 C9H11BO4, Product Details of C17H18N2O6.

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

Motornov, Vladimir published the artcileCopper(I)-Catalyzed Regioselective Chan-Lam N2-Vinylation of 1,2,3-Triazoles and Tetrazoles, Name: (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, the publication is Advanced Synthesis & Catalysis (2019), 361(14), 3306-3311, database is CAplus.

Copper-catalyzed coupling of π-deficient NH-azoles with vinylboronic acids or vinyltrifluoroborate salt provided a direct route to N2-vinyl-1,2,3-triazoles and N2-vinyltetrazoles. The coupling reaction was efficiently catalyzed by (phen)Cu(PPh₃)Br with low catalyst loading (5 mol%) under base-free conditions. The method was applicable for vinylation of unsubstituted, monosubstituted and disubstituted 1,2,3-triazoles with various functionalities with high N2-selectivity.

Advanced Synthesis & Catalysis published new progress about 844501-00-4. 844501-00-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Boronic Acids,Boronic acid and ester, name is (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, and the molecular formula is C10H18BNO4, Name: (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid.

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

Ulivieri, Alessandra published the artcileThyroid hormones regulate cardiac repolarization and QT-interval related gene expression in hiPSC cardiomyocytes, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, the publication is Scientific Reports (2022), 12(1), 568, database is CAplus and MEDLINE.

Prolongation of cardiac repolarization (QT interval) represents a dangerous and potentially life-threatening elec. event affecting the heart. Thyroid hormones (THs) are critical for cardiac development and heart function. However, little is known about THs influence on ventricular repolarization and controversial effects on QT prolongation are reported. Human iPSC-derived cardiomyocytes (hiPSC-CMs) and multielectrode array (MEA) systems were used to investigate the influence of 3,3′,5-triiodo-L-Thyronine (T3) and 3,3′,5,5′-tetraiodo-L-Thyronine (T4) on corrected Field Potential Duration (FPDc), the in vitro analog of QT interval, and on local extracellular Action Potential Duration (APD). Treatment with high THs doses induces a significant prolongation of both FPDc and APD, with the strongest increase reached after 24 h exposure. Preincubation with reverse T3 (rT3), a specific antagonist for nuclear TH receptor binding, significantly reduces T3 effects on FPDc, suggesting a TRs-mediated transcriptional mechanism. RNA-seq anal. showed significant deregulation in genes involved in cardiac repolarization pathways, including several QT-interval related genes. In conclusion, long-time administration of high THs doses induces FPDc prolongation in hiPSC-CMs probably through the modulation of genes linked to QT-interval regulation. These results open the way to investigate new potential diagnostic biomarkers and specific targeted therapies for cardiac repolarization dysfunctions.

Scientific Reports 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 C9H5Cl2F3, Name: Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.

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