Month: October 2022

Xu, Hai-Feng; Pan, You-Lu; Li, Gang-Jian; Hu, Xu-Yang; Chen, Jian-Zhong published the artcile< Copper(II)-Catalyzed Direct C-H (Hetero)arylation at the C3 Position of Indoles Assisted by a Removable N,N-Bidentate Auxiliary Moiety>, Electric Literature of 329214-79-1, the main research area is arylated indole regioselective preparation; indole arylboronic ester arylation copper catalyst.

The regioselective arylation of inert C3-H bonds in indoles reacting with arylboronates via effective copper-mediated catalysis with the aid of a facile and removable 2-pyridinylisopropyl (PIP) group without ligand participation was reported. This newly established method features high compatibility with diverse functional groups between coupling partners, including both indole substrates and arylboron reagents, consequentially leading to operational simplicity and providing access to generate the desired arylated products I [R = H, 4-Me, 5-MeO, 6-Br, etc.; R1 = Me, Bn; Ar = Ph, 2-thienyl, 3-pyridyl, etc.] in good to excellent yields of up to 97%. Synthetically, the PIP-derived amide moiety could subsequently be readily removed under mild reaction conditions to produce useful indolecarboxylic acids for further transformation.

Journal of Organic Chemistry published new progress about Amides, secondary Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Electric Literature of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Avci, Davut; Alturk, Sumeyye; Sonmez, Fatih; Tamer, Omer; Basoglu, Adil; Atalay, Yusuf; Zengin Kurt, Belma; Dege, Necmi published the artcile< A novel series of mixed-ligand M(II) complexes containing 2,2′-bipyridyl as potent α-glucosidase inhibitor: synthesis, crystal structure, DFT calculations, and molecular docking>, Application of C10H8N2, the main research area is 2,2′-Bipyridyl and 6-methylpyridine-2-carboxylic acid; DFT/HSE06; Docking; XRD, FT-IR and UV–Vis; α-Glucosidase.

Diabetes mellitus (DM) is a common degenerative disease and characterized by high blood glucose levels. Since the effective antidiabetic treatments attempt to decrease blood glucose levels, keeping glucose under control is very important. Recent studies have demonstrated that α-glucosidase inhibitor improves postprandial hyperglycemia and then reduces the risk of developing type 2 diabetes in patients. Therefore, the design and synthesis of high affinity glucosidase inhibitors are of great importance. In this regard, novel series of mixed-ligand M(II) complexes containing 2,2′-bipyridyl {[Hg(6-mpa)2(bpy)(OAc)]·2H2O, (1), [Co(6-mpa)2(bpy)2], (2), [Cu(6-mpa)(bpy)(NO3)]·3H2O, (3), [Mn(6-mpa)(bpy)(H2O)2], (4), [Ni(6-mpa)(bpy)(H2O)2]·H2O, (5), [Fe(6-mpa)(bpy)(H2O)2]·2H2O, (6), [Fe(3-mpa)(bpy)(H2O)2]·H2O, (7)} were synthesized as potential α-glucosidase inhibitors. Their effects on α-glucosidase activity were evaluated. All synthesized complexes displayed α-glucosidase inhibitory activity with IC50 values ranging from 0.184 ± 0.015 to > 600 μM. The exptl. spectral analyses were carried out using FT-IR and UV-Vis spectroscopic techniques for these complexes characterized by XRD and LC-MS/MS. Moreover, the calculations at d. functional theory approximation were used to obtain optimal mol. geometries, vibrational wavenumbers, electronic spectral behaviors, and major contributions to the electronic transitions for the complexes 1-7. Finally, to display interactions between the synthesized complexes and target protein (the template structure Saccharomyces cerevisiae isomaltase), the mol. docking study was carried out.

JBIC, Journal of Biological Inorganic Chemistry published new progress about 366-18-7. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Application of C10H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Catarineu, Noelle R.; Schoedel, Alexander; Urban, Philipp; Morla, Maureen B.; Trickett, Christopher A.; Yaghi, Omar M. published the artcile< Two Principles of Reticular Chemistry Uncovered in a Metal-Organic Framework of Heterotritopic Linkers and Infinite Secondary Building Units>, COA of Formula: C18H22BNO3, the main research area is zinc MOF heterotritopic benzoate benzosemiquinonate oxidopyridine linker solvothermal preparation; crystal structure zinc MOF heterotritopic benzoate benzosemiquinonate oxidopyridine linker; helicity zinc MOF heterotritopic benzoate benzosemiquinonate oxidopyridine linker.

Structural diversity of metal-organic frameworks (MOFs) was largely limited to linkers with at most two different types of coordinating groups. MOFs constructed from linkers with three or more nonidentical coordinating groups were not explored. Here, the authors report a robust and porous crystalline MOF, Zn3(PBSP)2 or MOF-910, constructed from a novel linker PBSP (phenylyne-1-benzoate, 3-benzosemiquinonate, 5-oxidopyridine) bearing three distinct types of coordinative functionality. The MOF adopts a complex and previously unreported topol. termed tto. The authors’ study suggests that simple, sym. linkers are not a necessity for formation of crystalline extended structures and that new, more complex topologies are attainable with irregular, heterotopic linkers. This work illustrates two principles of reticular chem.: first, selectivity for helical over straight rod secondary building units (SBUs) is achievable with polyheterotopic linkers, and second, the pitch of the resulting helical SBUs may be fine-tuned based on the metrics of the polyheterotopic linker.

Journal of the American Chemical Society published new progress about Crystal structure. 832735-54-3 belongs to class pyridine-derivatives, and the molecular formula is C18H22BNO3, COA of Formula: C18H22BNO3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kondori, Tahere; Akbarzadeh-T, Niloufar; Ghaznavi, Habib; Karimi, Zeinab; Shahraki, Jafar; Sheervalilou, Roghayeh; Shahraki, Omolbanin published the artcile< A binuclear iron(III) complex of 5,5′-dimethyl-2,2′-bipyridine as cytotoxic agent>, Recommanded Product: 2,2′-Bipyridine, the main research area is binuclear iron complex dimethyl bipyridine cytotoxic agent; 5,5′-dimethyl-2,2′-bipyridine; Binuclear iron(III) complex; Cytotoxicity; Fish salmon DNA.

The binuclear iron(III) complex (1), namely, {[Fe(5,5′-dmbpy)2(OH2)]2(O)}(NO3)4 with a distorted octahedral coordination, formed by four nitrogen and two oxygen atoms, was previously reported by our team. In this study the DNA-binding and cytotoxicity evaluation for target complex were studied. The results indicated strong cytotoxicity activity against A549 cells comparable to cisplatin values. The binding interaction between complex 1 and FS-DNA was investigated by UV-Vis, fluorescence spectroscopy, and gel electrophoresis at physiol. pH (7.2). The DNA binding investigation has shown groove binding interactions with complex 1, therefore the hydrogen binding plays an important role in the interaction of DNA with complex 1. The calculated thermodn. parameters (ΔH°, ΔS° and ΔG°) show that hydrogen bonding and Vander-Waals forces have an important function in Fe(III) complex-DNA interaction. Moreover, DNA cleavage was studied using agarose gel electrophoresis. Viscosity measurements illustrated that relative viscosity of DNA was unchanged with the adding concentrations of Fe(III) complex. Mol. docking simulation results confirmed the spectroscopic and viscosity titration outcomes.

BioMetals published new progress about Bicyclic aromatic hydrocarbons Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Recommanded Product: 2,2′-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Song, Jing-Ru; Li, Na; Li, Dian-Peng published the artcile< Synthesis and anti-proliferation activity of Mogrol derivatives bearing quinoline and triazole moieties>, Name: 3-Aminoisonicotinaldehyde, the main research area is Mogrol quinolinyl triazolyl synthesis antitumor agent; Lung cancer; Mogrol; Quinoline; Structural modification; Triazole.

A series of novel derivatives based on Mogrol were designed and synthesized in attempt to improve anti-lung cancer activity. The cytotoxicity against human lung cancer cells including A549 and NCI-H460 were performed by Cell Counting Kit-8 (CCK8) assay in vitro. The screening result showed that compound 8f exhibited the strongest activity with an IC50 value of 4.47μM against A549 cell, and could induce the cell apoptosis in a dose-dependent manner and arrest cell cycle at G0/G1 phase. Besides, compound 8f displayed anti-proliferation effect on A549 cell through inhibiting phosphorylation of signal transducer and activator of transcription 3 (STAT3). Furthermore, compared with Mogrol, compound 10a significantly improved the cytotoxicity against NCI-H460 with the IC50 value of 17.13μM. The research stimulated the development of potential therapeutic agent for lung cancer from the natural Mogrol.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 55279-29-3 belongs to class pyridine-derivatives, and the molecular formula is C6H6N2O, Name: 3-Aminoisonicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yuan, Qianjia; Prater, Matthew B.; Sigman, Matthew S. published the artcile< Enantioselective Synthesis of γ-Functionalized Cyclopentenones and β-Functionalized Cycloheptenones Utilizing a Redox-Relay Heck Strategy>, Electric Literature of 1416819-91-4, the main research area is gamma functionalized cyclopentenone enantioselective preparation; cyclopentenone aryl boronic acid alkenyl triflate palladium relay Heck; delta functionalized cycloheptenone enantioselective preparation; cycloheptenone aryl boronic acid alkenyl triflate palladium relay Heck; Asymmetric Catalysis; C–C Coupling; Heck Reaction; Palladium.

In this report, the desymmetrization of cyclic enones under relay Heck conditions with an array of aryl boronic acids, alkenyl triflates and indole derivatives was described. This method granted facile access to diverse γ-functionalized cyclopentenones I [Ar = Ph, 2-naphthyl, benzo[d][1,3]dioxol-5-yl, 4-oxocyclopent-2-en-1-yl, etc.] and δ-functionalized cycloheptenones II [R = Ph, 4-CF3C6H4, C(Me):C(Me)CO2Et, etc.]. Using this approach, a formal synthesis of (S)-baclofen was completed in high yield and excellent enantioselectivity.

Advanced Synthesis & Catalysis published new progress about Alkylation catalysts. 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Electric Literature of 1416819-91-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Hua; Liu, Jie; Qu, Jian-Ping; Kang, Yan-Biao published the artcile< Overcoming Electron-Withdrawing and Product-Inhibition Effects by Organocatalytic Aerobic Oxidation of Alkylpyridines and Related Alkylheteroarenes to Ketones>, Related Products of 350-03-8, the main research area is organocatalytic aerobic oxidation alkylpyridine alkylheteroarene.

An organocatalyzed aerobic benzylic C-H oxidation of alkyl and aryl heterocycles has been developed. This transition metal-free method is able to overcome the electron-withdrawing effect as well as product-inhibition effects in heterobenzylic radical oxidation A variety of ketones bearing N-heterocyclic groups could be prepared under relatively mild conditions with moderate to high yields.

Journal of Organic Chemistry published new progress about C-H bond activation (benzylic). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Related Products of 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Chengkai; Zhao, Yanqian; Li, Dandan; Liu, Jiejie; Han, Heguo; He, Daoyu; Tian, Xiaohe; Li, Shengli; Wu, Jieying; Tian, Yupeng published the artcile< Aggregation-induced emission (AIE)-active molecules bearing singlet oxygen generation activities: the tunable singlet-triplet energy gap matters>, HPLC of Formula: 350-03-8, the main research area is terpyridine quantum yield fluorescence aggregation induced emission UV.

Herein, a series of photosensitizers were constructed of α, β and γ-isomers of terpyridine and the corresponding N-methylation derivatives Benefiting from the tunable singlet-triplet energy gap and aggregation-induced emission characteristics, two-photon active photosensitizers L2b and L2c showed relatively strong intersystem crossing facilitating 1O2 generation and cell apoptosis with near-IR excitation.

Chemical Communications (Cambridge, United Kingdom) published new progress about Aggregation-induced emission. 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, HPLC of Formula: 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Stapleton, David; Gao, Guang; Michell, Belinda J.; Widmer, Jane; Mitchelhill, Ken; Teh, Trazel; House, Colin M.; Witters, Lee A.; Kemp, Bruce E. published the artcile< Mammalian 5'-AMP-activated protein kinase non-catalytic subunits are homologs of proteins that interact with yeast Snf1 protein kinase>, Name: 3-Bromo-1H-pyrrolo[3,2-c]pyridine, the main research area is AMP activated protein kinase subunit sequence; rat AMP activated protein kinase subunit; pig AMP activated protein kinase subunit; Snf1 kinase interacting protein homolog mammal; yeast CAT3 Snf4p homolog rat pig; Sip1p GAL38 yeast homolog rat pig.

The 5′-AMP-activated protein kinase is responsible for the regulation of fatty acid synthesis by phosphorylation and inactivation of acetyl-CoA carboxylase. The porcine liver 5′-AMP-activated protein kinase 63-kDa catalytic subunit co-purifies 14,000-fold with a 38- and 40-kDa protein (Mitchelhill, K. I. et al. (1994) J. Biol. Chem. 269, 2361-2364). The 63-kDa subunit is homologous to the Saccharomyces cerevisiae Snf1 protein kinase, which regulates gene expression during glucose derepression. Peptide amino acid and polymerase chain reaction-derived partial cDNA sequences of both the pig and rat liver enzymes show that the 38-kDa protein is homologous to Snf4p (CAT3) and that the 40-kDa protein is homologous to the Sip1p/Spm/GAL83 family of Snf1p interacting proteins. Sucrose d. gradient and crosslinking experiments with purified 5′-AMP-activated protein kinase suggest that both the 38- and 40- kDa proteins associate tightly with the 63-kDa catalytic polypeptide in either a heterotrimeric complex or in dimeric complexes. The 40-kDa subunit is autophosphorylated within the 63-kDa subunit complex. The sequence relationships between the mammalian 5′-AMP-activated protein kinase and yeast Snf1p extend to the subunit proteins consistent with conservation of the functional roles of these polypeptides in cellular regulation by this family of metabolite-sensing protein kinases.

Journal of Biological Chemistry published new progress about Phosphorylation, autophosphorylation. 23612-36-4 belongs to class pyridine-derivatives, and the molecular formula is C7H5BrN2, Name: 3-Bromo-1H-pyrrolo[3,2-c]pyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem