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One-step exchange-labelling of pyridines and other N-heteroaromatics using deuterium gas: catalysis by heterogeneous rhodium and ruthenium catalysts

A wide range of pyridines and other nitrogen heteroaromatics can be labelled with deuterium at room temperature and pressure by isotopic exchange with deuterium gas in THF in the presence of rhodium black, ruthenium black or 5% rhodium on alumina. The labelling is rapid, isotope efficient and applicable to both electron-rich and electron-poor substrates. In a few cases, a degree of reduction accompanies the exchange.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N30 – PubChem

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Structural basis for the role of mammalian aldehyde oxidases in the metabolism of drugs and xenobiotics

Aldehyde oxidases (AOXs) are molybdo-flavoenzymes characterized by broad substrate specificity, oxidizing aromatic/aliphatic aldehydes into the corresponding carboxylic acids and hydroxylating various heteroaromatic rings. Mammals are characterized by a complement of species-specific AOX isoenzymes, that varies from one in humans (AOX1) to four in rodents (AOX1, AOX2, AOX3 and AOX4). The physiological function of mammalian AOX isoenzymes is unknown, although human AOX1 is an emerging enzyme in phase-I drug metabolism. Indeed, the number of therapeutic molecules under development which act as AOX substrates is increasing. The recent crystallization and structure determination of human AOX1 as well as mouse AOX3 has brought new insights into the mechanisms underlying substrate/inhibitor binding as well as the catalytic activity of this class of enzymes.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N369 – PubChem

Extended knowledge of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 763114-26-7, and how the biochemistry of the body works.Computed Properties of C16H11FN2O3

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 763114-26-7, name is 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, introducing its new discovery. Computed Properties of C16H11FN2O3

DUAL INHIBITORS OF PARP1 AND CDK

Disclosed herein, in various embodiments, are compounds having dual activity as PARP1 and CDK inhibitors, and pharmaceutical compositions comprising the same. In some embodiments, the present disclosure provides for methods of treating diseases or conditions in a subject in need thereof, comprising administering one or more compounds disclosed herein. In some embodiment, the disease is cancer, including breast cancer.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N737 – PubChem

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Luminescent hydrido-carbonyl clusters of rhenium containing bridging 1,2-diazine ligands

The reaction of the electronically unsaturated (56 valence electrons, ve) tetrahedral cluster [Re4(mu3-H)4(CO) 12] (1) with pyridazine (pydz) gives as the main initial product the tetranuclear cluster [Re4(mu-H)4(mu-pydz)(pydz) 2(CO)12] (2a), with 64 ve and four hydrogen-bridged metal-metal interactions, with a spiked-triangle geometry. One of the three pydz ligands bridges, in a cis configuration, the cluster edge opposite to the vertex bearing the spike, as indicated by the X-ray single-crystal analysis. This species slowly decomposes, affording the dinuclear unsaturated (32 ve) complex [Re2(mu-H)2(mu-pydz)(CO)6] (3a) and two isomers of the tetranuclear cluster [Re4(mu-H) 4(mu-pydz)2-(CO)12] (64 ve), sharing an unusual square cluster geometry and differing in the trans (major, 85%, 4a) or cis (4a?) configuration of the bridging pydz ligands. The structures of 3a and 4a have been ascertained by X-ray analysis, while the characterization of 4a? was hampered by its instability (slowly transforming into 3a in THF solution). Both the dimer and the square cluster 4a are also formed directly (and quickly) from 1, being present in solution since the beginning of the reaction. Cluster 4a is the main final reaction product. The reaction with phthalazine follows a similar course, with some differences in the relative amount of the final products 3b and 4b. Most of the novel complexes are able to emit light in solution at room temperature, and photophysical measurements were performed in CH2Cl2 solution on the main stable reaction products (i.e., the dinuclear species 3a and 3b and the trans square clusters 4a and 4b). The emission was in the range of 580-645 nm, from MLCT excited states, with lifetimes on the order of a hundred nanoseconds (50-473 ns). The quantum yields were 1 order of magnitude higher for the squares (1.7 and 1.3% for 4a and 4b, respectively, in CH2Cl2) than for the dinuclear complexes (?0.1%). In the case of 4a, a blue shift and an increase of the emission intensity were observed upon decreasing the solvent polarity.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N331 – PubChem

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The one-pot synthesis of homoleptic phenylphthalazine iridium(III) complexes and their application in high efficiency OLEDs

A series of homoleptic cyclometalated iridium (III) complexes bearing a 1-phenylphthalazine framework have been synthesized with a facile one-pot method and characterized by X-ray single crystal diffraction. All complexes exhibited orange or red emission peaks at 583?623 nm with short lifetimes of 1.3?2.6 mus and high photoluminescence quantum yields of 41%?82%. These complexes exhibit good thermal stability with high Td of 275?394 C. The electronic states and orbital distributions of these iridium (III) complexes were studied by density functional theory. These complexes were used as emissive materials in Organic light-emitting diodes (OLEDs). The device based on 2 gave a peak current efficiency and external quantum efficiency (EQE) of 35.1 cd A?1 and 21.2%, respectively. The color coordinates of device based on 3 fully meet that of standard red of the National Television Standards Committee (NTSC). These results suggest that homoleptic phenylphthalazine iridium (III) complexes have potential application as efficient emitters in OLEDs.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N193 – PubChem

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Reference of 763114-26-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 763114-26-7, 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, introducing its new discovery.

LOW AFFINITY POLY(AD-RIBOSE) POLYMERASE 1 DEPENDENT CYTOTOXIC AGENTS

The present disclosure provides compounds of Formula (I) or (II), pharmaceutically acceptable salt, isotopic variant, stereoisomer, or a mixture thereof. Also provided are pharmaceutical compositions comprising a compound, methods of treating a poly(ADP-ribose)polymerase-1-mediated disease or disorder in a subject, methods of detecting a poly(ADP-ribose)polymerase-1-mediated neurodegenerative disease or disorder, or methods of monitoring cancer treatment in a subject. In some embodiments, the poly(ADP-ribose)polymerase-1-mediated disease or disorder is a neurodegenerative disease or cancer.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N751 – PubChem

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UHPLC-fluorescence method for the determination of trace levels of hydrazine in allopurinol and its formulations: Validation using total-error concept

The present approach poses an interesting way to quantify residues of the genotoxic impurity hydrazine in allopurinol and its pharmaceutical formulations using ultra high performance liquid chromatography coupled to fluorescence detection. Hydrazine was pre-column derivatized through a unique chemistry with o-phthalaldehyde under acidic conditions. Using highly acidic mobile phase the derivative exhibits a strong fluorescence intensity. Derivatization and chromatographic parameters were thoroughly investigated. The validation of the developed method has been carried out in the range of 10 to 200% of the target concentration limit of the analyte using the accuracy profiles as a graphical decision-making tool. The beta-expectation tolerance intervals did not exceed the acceptance criteria of ¡À20% which means that 95% of future results will be included in the defined bias limits. The variation of the relative bias ranged between ?6.0 and 0.5% and the RSD values for repeatability and intermediate precision were lower than 6.9% in all cases. The limit of detection (LOD) and the lower limit of quantification (LLOQ) were satisfactory and found to be 0.3 ng mL?1 (corresponding to 0.03 mug g?1 in solid sample). Experimental designs were constructed to study the robustness of the instrumental method and the derivatization procedure. The developed method has been successfully applied for the analysis of hydrazine in allopurinol API batches and tablets indicating that this methodology could be adopted from QC laboratories.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N112 – PubChem

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Lumonil compounds in criminal chemistry (a review)

DESPITE the development and progress in the detection of the significance of crimes, and after more than eighty years of discovery is a luminol is the basic chemical in the detection of crimes previously and now, was addressed the theoretical aspects of the compound of the luminol preparation methods and some of its chemical reactions as well as discuss the phenomenon of scintillation and transfer Energy, and then addressing some of the applications of chemical flash and receptor tests, DNA investigations were discussed, and the sensitivity of these reactions.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N575 – PubChem

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Neutrophil NET formation is regulated from the inside by myeloperoxidase-processed reactive oxygen species

Aim Neutrophil extracellular traps (NETs) are mesh-like DNA fibers clad with intracellular proteins that are cast out from neutrophils in response to certain stimuli. The process is thought to depend on reactive oxygen species (ROS) generated by the phagocyte NADPH-oxidase and the ROS-modulating granule enzyme myeloperoxidase (MPO), but when, how, and where these factors contribute is so far uncertain. The neutrophil NADPH-oxidase can be activated at different cellular sites and ROS may be produced and processed by MPO within intracellular granules, even in situations where a phagosome is not formed, e.g., upon stimulation with phorbol myristate acetate (PMA). Objectives We investigated the subcellular location of ROS production and processing by MPO in the context of PMA-induced NET formation. Results Complete neutralization of extracellular ROS was not sufficient to block NET formation triggered by PMA, indicating that intragranular ROS are critical for NETosis. Employing a set of novel MPO-inhibitors, inhibition of NET formation correlated with inhibition of intragranular MPO activity. Also, extracellular addition of MPO was not sufficient to rescue NET formation in completely MPO-deficient neutrophils and specific neutralization by luminol of MPO-processed ROS within intracellular granules led to a complete block of PMA-triggered NET formation. Conclusion We show for the first time that inhibition of intragranular MPO activity, or neutralization of intragranular MPO-processed ROS by luminol effectively block NET formation. Our data demonstrate that ROS must be formed and processed by MPO in order to trigger NET formation, and that these events have to occur within intracellular granules.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N529 – PubChem

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Synthesis, structure, and in vitro anticancer activity of new polycyclic 1,2-diazines

The synthesis, structure, and in vitro anticancer activity of a new class of anticancer derivatives with dihydrobenzo[5,6]isoindolo[1,2-A]phthalazine and dihydrobenzo[f]pyridazino[6,1-A]isoindole skeletons are presented. The preparation is straight and efficient, involving two steps only: a N-Alkylation of the pyridazine or phthalazine heterocycle, followed by a [3 + 2] dipolar cycloaddition of 1,2-diazinium ylides to the corresponding dipolarophiles. The synthesis was performed under microwave and ultrasound (US) irradiation as well as under conventional thermal heating. The most effective conditions in term of yields and time were found to be US irradiation. The penta- and tetra-cyclic 1,2-diazines were evaluated for their in vitro anticancer activity. The pentacyclic 1,2-diazine derivatives exhibit a significant anticancer activity against Non-Small Cell Lung Cancer NCI-H460, Leukemia MOLT-4, Leukemia CCRF-CEM, and Breast Cancer MCF7. A feasible explanation for anticancer efficiency of the pentacyclic 1,2-diazines have been furnished, being correlated with the mechanisms of action. Graphical Abstract: The synthesis (conventional thermal heating, microwave and ultrasound irradiation), structure, and in vitro anticancer activity of a new class of anticancer molecules with polycyclic 1,2-diazines skeleton is presented.[Figure not available: see fulltext.]

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N278 – PubChem