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Six-Membered Ring Systems: Diazines and Benzo Derivatives

Found in natural products, and frequently used as flavoring agents or as building blocks for pharmaceuticals, diazines and their benzo derivatives possess a diverse set of properties, allowing a broad range of applications, spanning from medicinal chemistry to electrochemistry. New diazine-based natural products continue to be isolated and studied. In addition, new syntheses, reactions, and applications of diazine-based compounds are reported every year. Recent advances in the development of new preparations, reactions, and applications of diazines and their benzo derivatives, published in the literature in 2018, are discussed in this review.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N364 – PubChem

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Electrochemical Reductive Carboxylation: Reduction of Unsaturated Compounds in the Presence of Methyl Chloroformate

Mono- and dicarboxylated derivatives have been obtained by electroreduction of various unsaturated compounds in acetonitrile at a mercury-pool cathode in the presence of methyl chloroformate.Unsaturated compounds included activated olefins, ketones, aromatic Schiff bases, nitro compounds, and nitrogen heterocycles.The distribution of the products and their yields depend on the nature of the supporting electrolyte (Et4NClO4 or LiClO4).Reduction mechanisms accounting for the nature of the reduction products are proposed on the basis of voltammetric and coulometric data.In some cases it is possible to obtain the kinetic parameters.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N42 – PubChem

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Synthetic Route of 72702-95-5, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.72702-95-5, Name is 2-(3-(4-Bromo-2-fluorobenzyl)-4-oxo-3,4-dihydrophthalazin-1-yl)acetic acid, molecular formula is C17H12BrFN2O3. In a article£¬once mentioned of 72702-95-5

Calibration of the Heat Flow and Physical Properties Package (HP 3) for the InSight Mars Mission

The (HP3) of the InSight Mars mission is an instrument package to measure the Martian geothermal heat flow. The instrument’s platinum resistance temperature sensors have been calibrated between -75 and +55?C, and the absolute temperature uncertainty of the calibration is 10?mK. Temperature differences can be measured with an uncertainty of better than 5?mK. HP3 determines regolith thermal conductivity by using the HP3 mole as a modified line heat source, and thermal conductivity can be measured with an uncertainty of better than 4%. Tilt sensors used to determine the attitude of the mole during penetration measure tilt with an uncertainty of better than 0.25.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N864 – PubChem

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253-52-1, Name is Phthalazine, belongs to phthalazine compound, is a common compound. Computed Properties of C8H6N2In an article, once mentioned the new application about 253-52-1.

Intramolecular Cyclization via Onium Salts. A Novel Synthesis of 1,3-Thiazolidines from Chloromethyl (Trimethylsilyl)methyl Sulfide and Nitrogen-Containing Heteroaromatic Compounds

Polycyclic 1,3-thiazolidines were prepared by the fluoride ion promoted desilylation, followed by intramolecular 1,5-cyclization, of onium salts derived from the sulfide 1 and a variety of heteroaromatics.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N189 – PubChem

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Substrate-induced up-regulation of aldose reductase by methylglyoxal, a reactive oxoaldehyde elevated in diabetes

Methylglyoxal (MG), a reactive dicarbonyl produced during glucose metabolism, induced a dose- and time-dependent increase in aldose reductase (AR) mRNA level in rat aortic smooth muscle cells (SMCs). AR has been implicated in the pathogenesis of diabetic complications, whereas the clinical efficacy of AR inhibitors has not been unequivocally proven. The enzyme catalyzes the reduction of glucose in the polyol pathway, as well as that of MG, which is known to be a preferred substrate of AR. A maximum of 4.5-fold induction of AR mRNA by MG was accompanied by elevated enzyme activity and protein levels and was completely abolished in the presence of cycloheximide or actinomycin D. Pretreatment of SMCs with N-acetyl-L-cysteine significantly suppressed the MG-induced AR expression, whereas DL-buthionine-(S,R)-sulfoximine further augmented the MG-induced increase in AR mRNA level. Intracellular levels of reactive oxygen species determined using 2?,7?-dichlorofluorescein diacetate were significantly elevated in SMCs treated with MG, suggesting the involvement of oxidative stress in this process. However, inconsistent with our previous findings on oxidative stress-induced up-regulation of AR, the inhibition of extracellular signal- regulated kinase by 2?-amino-3?-methoxyflavone (PD98059) did not affect MG-induced AR expression, whereas blockade of the p38 mitogen-activated protein kinase pathway by 4-(4-fluorophenyl)-2-(4-methylsulfonylphenyl)-5-(4-pyridyl) imidazol (SB203580) significantly suppressed the induction. The cytotoxic effect of MG on SMCs was significantly enhanced in the presence of the AR inhibitor ponalrestat, indicating a protective role of AR against MG-induced cell damage. Taken together, these observations indicated that substrate-induced induction of AR by MG during hyperglycemic conditions may hinder vascular remodeling and accelerate the development of vascular lesions in diabetes.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N854 – PubChem

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Phthalazin-1(2H)-one as a remarkable scaffold in drug discovery

Phthalazinones are an important kind of nitrogen atom containing heterocyclic compounds due to their synthetic and pharmacological versatility. This fused heterocycle system represents a common structural feature for many bioactive compounds showing a variety of pharmacological activities such as anticancer, anti-diabetic, anti-asthmatic, antihistaminic, antihypertensive, antithrombotic, anti-inflammatory, analgesic, antidepressant or antimicrobial agents, which makes it an attractive scaffold for the design and development of new drugs. This review summarizes detailed and updated information, described in recent non-patent literature, about the most relevant pharmacological properties of phthalazinone derivatives, highlighting the application of this potent pharmacophore in drug discovery.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N923 – PubChem

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Increased intracellular and extracellular oxidant production in phagocytes of rheumatic patients treated with biological therapy – Whole blood quantification

Infectious complications, resulting from reduced activity of immune cells, are the most severe and common adverse effects of biological therapy. This study analyzed the effect of biological therapy on blood phagocytes, focusing on the formation of reactive oxygen species (ROS), an important factor in the defence against invading pathogens. Intra- and extracellular ROS production were recorded separately, on the basis of luminol and isoluminol chemiluminescence in patients treated with antibodies against tumor necrosis factor-alpha or against interleukin-6 receptor. In comparison to healthy donors or to rheumatic patients treated with classical immunosuppressive drugs, biological therapy increased ROS formation in both compartments. This indicates that the anti-microbial activity of blood phagocytes was not reduced by TNFalpha- or IL-6-neutralizing therapy, at least in terms of ROS. The method presented does not require blood fractionation, which could modify activity of phagocytes and cause loss of some sub-populations of these cells. The technique is simple, requires microliter volumes of blood and is thus well applicable to clinical studies.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N577 – PubChem

Brief introduction of Phthalazine

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Diazaarynes: 3,4- and 4,5-Didehydropyridazine By Electron Impact and Thermolytic Fragmentation of The Corresponding Dicarboxylic Anhydrides

The new hetarynes (1) and (2) heve been advanced as intermediates in the vapour phase both for the electron impact and the pyrolytic fragmentation pattern of pyridazine-3,4- and 4,5-dicarboxylic acid anhydrides (10) and (11), respectively.The presence of a peak at m/e 78 in the mass spectra of these compounds, as well as the formation of the diazanaphtalenes (12) and (13), respectively, from their thermolysis in benzene, appeared to support this proposal.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N412 – PubChem

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Surface-Enhanced Raman Spectra of Phthalazine. Anion-Induced Reorientation on a Silver Electrode

A remarkable potential-dependent SERS of phthalazine adsorbed on a silver electrode has been observed from a series of aqueous solutions containing Cl-, I-, Br-, F-, SCN-, SO42-, or ClO4- as electrolyte anion.The Raman intensity of certain b2 modes was greatly enhanced accompanied by anion desorption during the cathodic sweep.However, the b2 species were absent from the SER spectra when the surfaces were fully covered with anions.The specific adsorption of anions influences the orientations of the adsorbed phthalazine.The importance of the charge-transfer effect on SERS is also suggested from the potential and excitation-wavelength-dependent spectral changes.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N431 – PubChem

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The reactions of 2-(chloroseleno)benzoyl chloride with pyridine and related azines

The reaction of 2-(chloroseleno)benzoyl chloride with pyridine and pyridine-like heterocycles such as pyrimidine, pyrazine, quinoline, phthalazine, phenazine and 1,10-phenanthroline was studied. In the most cases stable 2-(hydroxyseleno)benzoylazinium chlorides were produced depending on the number of the pyridinium-like nitrogen atoms and their situation in the ring system.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N327 – PubChem