Month: December 2022

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

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

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

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

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

Guan, Aiying published the artcileN-Phenyl heteroarylamine analogues of fluazinam using the intermediate derivatization methods approach, Recommanded Product: 2-Bromopyridin-3-amine, the publication is Journal of Chemical Sciences (Bangalore, India) (2014), 126(4), 1107-1114, database is CAplus.

Twenty-one N-Ph heteroarylamine analogs of fluazinam were prepared via nucleophilic substitution reaction of 2,6-dichloro-3,5-dinitrotoluene with heteroarylamines using the intermediate derivatization method. 2,6-Dichloro-3,5-dinitrotoluene, the key intermediate, was synthesized by nitration of 2,6-dichlorotoluene. Preliminary bioassays indicated that most of the compounds showed good fungicidal activity against rice blast. The activity of I was equal to that of fluazinam. The relationship between mol. structure and biol. activity suggested that introduction of electron-withdrawing groups in the pyridine ring was important for optimizing fungicidal activity against rice blast.

Journal of Chemical Sciences (Bangalore, India) 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

Wang, Peng published the artcileLigand-Promoted meta-C-H Amination and Alkynylation, Application of 3-Amino-5-(trifluoromethyl)pyridin-2-ol, the publication is Journal of the American Chemical Society (2016), 138(42), 14092-14099, database is CAplus and MEDLINE.

Using a modified norbornene (Me bicyclo[2.2.1]hept-2-ene-2-carboxylate) as a transient mediator, meta-C-H amination and meta-C-H alkynylation of aniline and phenol substrates have been developed for the first time. Both the identification of a monoprotected 3-amino-2-hydroxypyridine/pyridone-type ligand and the use of a modified norbornene as a mediator are crucial for the realization of these two unprecedented meta-C-H transformations. A variety of substrates are compatible with both meta-C-H amination and meta-C-H alkynylation. Amination and alkynylation of heterocyclic substrates including indole, indoline, and indazole afford the desired products in moderate to high yields.

Journal of the American Chemical Society published new progress about 90778-25-9. 90778-25-9 belongs to pyridine-derivatives, auxiliary class Trifluoromethyl,Pyridine,Fluoride,Amine,Alcohol, name is 3-Amino-5-(trifluoromethyl)pyridin-2-ol, and the molecular formula is C6H8O4, Application of 3-Amino-5-(trifluoromethyl)pyridin-2-ol.

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

Yang, Xiaobao published the artcileStructure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors, Formula: C5H6BNO2, the publication is Journal of Medicinal Chemistry (2016), 59(16), 7617-7633, database is CAplus and MEDLINE.

EZH2 or EZH1 (enhancer of zeste homolog 2 or 1) is the catalytic subunit of polycomb repressive complex 2 (PRC2) that catalyzes methylation of histone H3 lysine 27 (H3K27). PRC2 hyperactivity and/or hypertrimethylation of H3K27 are associated with numerous human cancers, therefore inhibition of PRC2 complex has emerged as a promising therapeutic approach. Recent studies have shown that EZH2 and EZH1 are not functionally redundant and inhibition of both EZH2 and EZH1 is necessary to block the progression of certain cancers such as MLL (mixed-lineage leukemia)-rearranged leukemias. Despite the significant advances in discovery of EZH2 inhibitors, there has not been a systematic structure-activity relation (SAR) study to investigate the selectivity between EZH2 and EZH1 inhibition. Here, the authors report the authors SAR studies that focus on modifications to various regions of the EZH2/1 inhibitor UNC1999 (5) to investigate the impact of the structural changes on EZH2 and EZH1 inhibition and selectivity.

Journal of Medicinal Chemistry 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 C13H18BClO3, Formula: C5H6BNO2.

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

Wu, Zi-Zhen published the artcileAminopyridines Potentiate Synaptic and Neuromuscular Transmission by Targeting the Voltage-activated Calcium Channel β Subunit, Application In Synthesis of 18437-58-6, the publication is Journal of Biological Chemistry (2009), 284(52), 36453-36461, database is CAplus and MEDLINE.

Aminopyridines such as 4-aminopyridine (4-AP) are widely used as voltage-activated K⁺ (Kv) channel blockers and can improve neuromuscular function in patients with spinal cord injury, myasthenia gravis, or multiple sclerosis. Here, we present novel evidence that 4-AP and several of its analogs directly stimulate high voltage-activated Ca²⁺ channels (HVACCs) in acutely dissociated neurons. 4-AP, 4-(aminomethyl)pyridine, 4-(methylamino)pyridine, and 4-di(methylamino)pyridine profoundly increased HVACC, but not T-type, currents in dissociated neurons from the rat dorsal root ganglion, superior cervical ganglion, and hippocampus. The widely used Kv channel blockers, including tetraethylammonium, α-dendrotoxin, phrixotoxin-2, and BDS-I, did not mimic or alter the effect of 4-AP on HVACCs. In HEK293 cells expressing various combinations of N-type (Cav2.2) channel subunits, 4-AP potentiated Ca²⁺ currents primarily through the intracellular β₃ subunit. In contrast, 4-AP had no effect on Cav3.2 channels expressed in HEK293 cells. Furthermore, blocking Kv channels did not mimic or change the potentiating effects of 4-AP on neurotransmitter release from sensory and motor nerve terminals. Thus, our findings challenge the conventional view that 4-AP facilitates synaptic and neuromuscular transmission by blocking Kv channels. Aminopyridines can directly target presynaptic HVACCs to potentiate neurotransmitter release independent of Kv channels.

Journal of Biological 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 C9H6N2O4, Application In Synthesis of 18437-58-6.

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

Liu, Tao published the artcileStraightforward installation of carbon-halogen, carbon-oxygen and carbon-carbon bonds within metal-organic frameworks (MOF) via palladium-catalyzed direct C-H functionalization, Application In Synthesis of 85237-71-4, the publication is Chemical Communications (Cambridge, United Kingdom) (2014), 50(87), 13261-13264, database is CAplus and MEDLINE.

The straightforward C-H functionalization of UiO-67-dcppy materials, was realized by a Pd-catalyzed PSM. This novel protocol provides an efficient method for the synthesis of various functionalized MOFs, which showed promising adsorbent ability in removing phenolic contaminates from water.

Chemical Communications (Cambridge, United Kingdom) published new progress about 85237-71-4. 85237-71-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is 5-Methyl-2-(p-tolyl)pyridine, and the molecular formula is C13H13N, Application In Synthesis of 85237-71-4.

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