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Application of 1452-77-3. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Switching the secondary and natural activity of Nitrilase from Acidovorax facilis 72 W for the efficient production of 2-picolinamide. Author is Wang, Liuzhu; Jiang, Shuiqin; Sun, Yangyang; Yang, Zeyu; Chen, Zhi; Wang, Hualei; Wei, Dongzhi.

Catalytic promiscuity, or the ability to catalyze a secondary reaction, provides new opportunities for industrial biocatalysis by expanding the range of biocatalytic reactions. Some nitrilases converting nitriles to amides, referred to as the secondary activity, show great potential for amides production And our goal was exploiting the amide-forming potential of nitrilases. In this study, we characterized and altered the secondary activity of nitrilase from Acidovorax facilis 72 W (Nit72W) towards different substrates. We increased the secondary activity of Nit72W towards 2-cyanopyridine by 196-fold and created activity toward benzonitrile and p-nitrophenylacetonitrile by modifying the active pocket. Surprisingly, the best mutant, W188M, completely converted 250 mM 2-cyanopyridine to more than 98% 2-picolinamide in 12 h with a specific activity of 90 U/mg and showed potential for industrial applications. Nit72W was modified to increase its secondary activity for the amides production, especially 2-picolinamide.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 1452-77-3, is researched, Molecular C6H6N2O, about Characterization of copper(II) specific pyridine containing ligands: Potential metallophores for Alzheimer’s disease therapy, the main research direction is copper zinc pyridinylmethylpicolinamide pyridinylmethylpyridinylmethylamino complex formation ESR; Amyloid β; Copper; Electron Paramagnetic Resonance spectroscopy; Metallophore; Reactive oxygen species; Speciation.Reference of Picolinamide.

Two amide group containing pyridine derivatives, N-(pyridin-2-ylmethyl)picolinamide (PMPA) and N-(pyridin-2-ylmethyl)-2-((pyridin-2-ylmethyl)amino)acetamide (DPMGA), have been investigated as potential metallo-phores in the therapy of Alzheimer’s disease. Their complex formation with Cu(II) and Zn(II) were characterized in details. Unexpectedly not only the Cu(II) but also the Zn(II) was able to induce deprotonation of the amide-NH, however, it occurred only at higher pH or at higher metal ion concentrations than the biol. conditions. At μM concentration level mono complexes (MLH-1) dominate with both ligands. Direct fluorescence and reactive oxygen species (ROS) producing measurements prove that both ligands are able to remove Cu(II) from its amyloid-β complexes (CuAβ). Correlation was also established between the conditional stability constant of the Cu(II) complexes with different ligands and their ability of inhibition of ROS production by CuAβ.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Picolinamide( cas:1452-77-3 ) is researched.COA of Formula: C6H6N2O.Della Volpe, S.; Linciano, P.; Listro, R.; Tumminelli, E.; Amadio, M.; Bonomo, I.; Elgaher, W. A. M.; Adam, S.; Hirsch, A. K. H.; Boeckler, F. M.; Vasile, F.; Rossi, D.; Collina, S. published the article 《Identification of N,N-arylalkyl-picolinamide derivatives targeting the RNA-binding protein HuR, by combining biophysical fragment-screening and molecular hybridization》 about this compound( cas:1452-77-3 ) in Bioorganic Chemistry. Keywords: Fragment screening; Ligand-protein interaction; Molecular docking; RNA-binding proteins; SPR; STD-NMR. Let’s learn more about this compound (cas:1452-77-3).

Hu proteins are members of the RNA-binding protein (RBP) family and play a pivotal role in the regulation of post-transcriptional processes. Through interaction with selected mRNAs, RBPs regulate their function and stability; as a consequence, RBP dysregulation can cause abnormal translation of key proteins involved in several pathologies. In the past few years, this observation has sparked interest to develop new treatments against these pathologies by using small mols. able to modulate RBP activity. Among the four Hu proteins, we have directed our efforts towards the isoform HuR, which is mainly involved in cancer, inflammation and retinopathy. Aimed at developing compounds able to modulate the stability of HuR-mRNA complexes, in the present work, we applied a biophys. fragment screening by assessing a library of halogen-enriched heterocyclic fragments (HEFLibs) via Surface Plasmon Resonance (SPR) and Saturation Transfer Difference (STD) NMR to select promising fragments able to interact with HuR. One selected fragment and a few com. available congeners were exploited to design and synthesize focused analogs of compound N-(3-chlorobenzyl)-N-(3,5-dihydroxyphenethyl)-4-hydroxybenzamide (1), our previously reported hit. STD NMR spectroscopy, mol. modeling, and SPR offered further insight into the HuR-small mol. interaction and showed that fragment-based approaches represent a promising and yet underexplored strategy to tackle such unusual targets. Lastly, fluorescence polarization (FP) studies revealed the capability of the new compounds to interfere with the formation of the HuR-mRNA complex. This is, to our knowledge, the first fragment-based campaign performed on the Hu protein class, and one of the few examples in the larger RBP field and constitutes an important step in the quest for the rational modulation of RBPs and related RNA functions by small mols.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Picolinamide( cas:1452-77-3 ) is researched.Electric Literature of C6H6N2O.Nie, Zimeng; Yan, Binghua; Xu, Yunhai; Awasthi, Mukesh Kumar; Yang, Haijun published the article 《Characterization of pyridine biodegradation by two Enterobacter sp. strains immobilized on Solidago canadensis L. stem derived biochar》 about this compound( cas:1452-77-3 ) in Journal of Hazardous Materials. Keywords: pyridine biodegradation wastewater treatment morphol phys chem property; Biodegradation; Immobilization; Intermediates; Metabolic pathway; Mineralization. Let’s learn more about this compound (cas:1452-77-3).

In this study, two pyridine-degrading strains namely Enterobacter cloacae complex sp. BD17 and Enterobacter sp. BD19 were isolated from the aerobic tank of a pesticide wastewater treatment plant. The mixed bacteria H4 composed of BD17 and BD19 at a ratio of 1:1 was immobilized by Solidago canadensis L. stem biochar with a dosage of 2 g·L–1. The highest pyridine removal rate of 91.70% was achieved by the immobilized H4 at an initial pyridine concentration of 200 mg·L-1, pH of 7.0, temperature of 28°C and salinity of 3.0% within 36 h. The main intermediates of pyridine degradation by BD17 were pyridine-2-carboxamide, 2-aminopropanediamide, and 2-aminoacetamide, while 2-picolinic acid, iso-Pr acetate, iso-Pr alc., and acetaldehyde were identified with BD19 by adopting GC-MS technique. Interestingly, there was a possibility of totally mineralization of pyridine and the corresponding degradation pathways of BD17 and BD19 were revealed for the first time.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Asian Journal of Organic Chemistry called Picolinamide-Based Iridium Catalysts for Aqueous Formic Acid Dehydrogenation: Increase in Electron Density of Amide N through Substituents, Author is Guo, Jian; Yin, Chengkai; Li, Maoliang; Zhong, Dulin; Zhang, Yuguan; Li, Xiaobin; Wang, Yilin; Yao, Hong; Qi, Tiangui, which mentions a compound: 1452-77-3, SMILESS is O=C(N)C1=NC=CC=C1, Molecular C6H6N2O, Related Products of 1452-77-3.

Formic acid (FA) is considered to be a potential hydrogen storage material. Homogeneous catalysts are desired, which decompose aqueous FA into H2 and CO2 without addition of organic additives as they can contaminate the generated gas mixture We report a new series of Cp*Ir (Cp*=pentamethylcyclopentadienyl) catalysts featuring picolinamide-based ligands for efficient H2 generation from FA solution Among them in-situ generated catalyst from [Cp*Ir(H2O)3]SO4 and picolinohydroxamic acid (L3) achieved a high turnover frequency (TOF) of 90625 h-1 at 80 °C in 0.9 M FA solution and a turnover number (TON) of 120520 at 80 °C in a recycle experiment The substituent effect of amide N atom was discussed and a plausible mechanism was proposed based on the exptl. results.

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Related Products of 1452-77-3. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Improving Compliance and Decreasing Drug Accumulation of Diethylstilbestrol through Cocrystallization. Author is Li, Zhen; Li, Meiqi; Peng, Bo; Zhu, Bingqing; Wang, Jian-rong; Mei, Xuefeng.

Diethylstilbestrol (DES), a synthetic nonsteroidal estrogen, has been prescribed for advanced breast cancer and prostate cancer. However, its poor compliance, reactive metabolite toxicity and hydrophobicity-induced drug accumulation has limited its applications. In this study, we aimed to modulate its dissolution rate and reduce reactive metabolites and drug accumulation through cocrystn. Cocrystals of DES with isonicotinamide (INA), picolinamide (PIN), nicotinamide (NIA), urea (UREA), sarcosine (SAR), and flavone (FLA) were obtained. Different crystallization strategies result in cocrystal polymorphs for DES with INA and FLA. Intrinsic dissolution rate (IDR) characterizations in pH 2.0 buffer solution were conducted. Two assumptions (enhancing Cmax or prolonging Tmax) with the aim of improving compliance were put forward. On the basis of the IDR results (DES-NIA with a 1.5-fold increase in IDR and DES-2FLA-B with a 5.5-fold decrease in IDR) and the pharmacol. activities of coformers (NIA and FLA with CYPs inhibition and UGTs stimulation effects), the pharmacokinetic behaviors of these two cocrystals were further researched. The 2-fold prolongation of Tmax in the PK profile DES-2FLA-B facilitated an improvement in compliance. In addition, the higher clearance rates and the potential to reduce oxidative metabolites in DES-2FLA-B help to decrease the drug accumulation and reduce the adverse effects of DES.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Highly Efficient Synthesis of Alkyl N-Arylcarbamates from CO2, Anilines, and Branched Alcohols with a Catalyst System of CeO2 and 2-Cyanopyridine, the main research direction is arylcarbamate preparation; carbon dioxide aniline alc multicomponent reaction cerium dioxide catalyst.Related Products of 1452-77-3.

Highly efficient synthesis of alkyl N-arylcarbamates from CO2, anilines, and alcs. using the CeO2 and 2-cyanopyridine catalyst system was substantiated by selecting branched alcs., such as 2-propanol and cyclohexanol, with minimized formation of byproducts, such as dialkyl carbonates and picolinamide. The catalyst system is operable even at low CO2 pressure (≤1 MPa), and the target carbamates were obtained with high arylamine-based yields (up to 94%). Alkyl N-phenylcarbamates were obtained from CO2, anilines, and alcs. with high yield and minimized formation of byproducts by using branched alcs.

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Electric Literature of C6H6N2O. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Characterization of pyridine biodegradation by two Enterobacter sp. strains immobilized on Solidago canadensis L. stem derived biochar. Author is Nie, Zimeng; Yan, Binghua; Xu, Yunhai; Awasthi, Mukesh Kumar; Yang, Haijun.

In this study, two pyridine-degrading strains namely Enterobacter cloacae complex sp. BD17 and Enterobacter sp. BD19 were isolated from the aerobic tank of a pesticide wastewater treatment plant. The mixed bacteria H4 composed of BD17 and BD19 at a ratio of 1:1 was immobilized by Solidago canadensis L. stem biochar with a dosage of 2 g·L–1. The highest pyridine removal rate of 91.70% was achieved by the immobilized H4 at an initial pyridine concentration of 200 mg·L-1, pH of 7.0, temperature of 28°C and salinity of 3.0% within 36 h. The main intermediates of pyridine degradation by BD17 were pyridine-2-carboxamide, 2-aminopropanediamide, and 2-aminoacetamide, while 2-picolinic acid, iso-Pr acetate, iso-Pr alc., and acetaldehyde were identified with BD19 by adopting GC-MS technique. Interestingly, there was a possibility of totally mineralization of pyridine and the corresponding degradation pathways of BD17 and BD19 were revealed for the first time.

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Kumata, Katsushi; Hatori, Akiko; Yamasaki, Tomoteru; Zhang, Yiding; Mori, Wakana; Fujinaga, Masayuki; Xie, Lin; Nengaki, Nobuki; Zhang, Ming-Rong published the article 《Synthesis and evaluation of 4-(2-fluoro-4-[11C]methoxyphenyl)-5-((2-methylpyridin-4-yl)methoxy)picolinamide for PET imaging of the metabotropic glutamate receptor 2 in the rat brain》. Keywords: carbon 11 fluoromethoxyphenyl methylpyridinyl methoxypicolinamide preparation brain mGluR2 PET; In vitro autoradiography; Metabotropic glutamate receptor 2; Positron emission tomography; Radiotracer; Schizophrenia.They researched the compound: Picolinamide( cas:1452-77-3 ).Application In Synthesis of Picolinamide. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:1452-77-3) here.

Metabotropic glutamate receptor 2 (mGluR2) has been suggested as a therapeutic target for treating schizophrenia-like symptoms arising from increased glutamate transmission in the human forebrain. However, no reliable positron emission tomog. (PET) radiotracer allowing for in vivo visualization of mGluR2 in the human brain is currently available. In this study, we synthesized 4-(2-fluoro-4-[11C]methoxyphenyl)-5-((2-methylpyridin-4-yl)methoxy)picolinamide ([11C]1) and evaluated its potential as a PET tracer for imaging mGluR2 in the rodent brain. Compound 1, a neg. allosteric modulator (NAM) of mGluR2, showed high in vitro binding affinity (IC50: 26 nM) for mGluR2 overexpressed in human cells. [11C]1 was synthesized by O-[11C]methylation of the phenol precursor 2 with [11C]methyl iodide. After the reaction, HPLC purification and formulation, [11C]1 of 7.4 ± 2.8 GBq (n = 8) was obtained from [11C]carbon dioxide of 22.5 ± 4.8 GBq (n = 8) with >99% radiochem. purity and 70 ± 32 GBq/μmol (n = 8) molar activity at the end of synthesis. In vitro autoradiog. for rat brains showed that [11C]1 binding was heterogeneously distributed in the cerebral cortex, striatum, hippocampus, and cerebellum. This pattern is consistent with the regional distribution pattern of mGluR2 in the rodent brain. The radioactivity was significantly reduced by self- or MNI-137 (a mGluR2 NAM) blocking. Small-animal PET studies indicated a low in vivo specific binding of [11C]1 in the rat brain. The brain uptake was increased in a P-glycoprotein and breast cancer resistant protein double knockout mouse, when compared to a wild-type mouse. While [11C]1 presented limited potential as an in vivo PET tracer for mGluR2, we suggested that it can be used as a lead compound for developing new radiotracers with improved in vivo brain properties.

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Recommanded Product: Picolinamide. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Picolinamide, is researched, Molecular C6H6N2O, CAS is 1452-77-3, about Phase Transfer Ceria-Supported Nanocatalyst for Nitrile Hydration Reaction. Author is Gupta, Nikitra N.; Punekar, Amrin S.; Raj, Karthik Raja E. K.; Ghodekar, Medha M.; Patil, Vipul S.; Gopinath, Chinnakonda S.; Raja, Thirumalaiswamy.

The present study elaborates the catalytic effect of rare-earth metal oxides (Sm2O3 and La2O3) over ceria as a support phase transfer catalyst. The synthesized catalysts have been subjected to different characterization techniques, such as field-emission SEM, high-resolution transmission electron microscopy, powder X-ray diffraction, N2 adsorption-desorption (BET surface anal.), temperature-programmed desorption study (NH3/CO2-TPD), Fourier transform IR, Raman anal., and XPS to get better insights into the catalytic activity of the catalysts for hydration of nitrile.

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