Month: March 2021

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NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N696 – PubChem

3682-14-2, Name is 6-Amino-2,3-dihydrophthalazine-1,4-dione, belongs to phthalazine compound, is a common compound. Computed Properties of C8H7N3O2In an article, once mentioned the new application about 3682-14-2.

A Ganoderma-Derived Compound Exerts Inhibitory Effect Through Formyl Peptide Receptor 2

Formyl peptide receptors (FPRs) are G protein-coupled receptors (GPCRs) widely expressed in neutrophils and other phagocytes. FPRs play important roles in host defense, inflammation, and the pathogenesis of infectious and inflammatory diseases. Because of these functions, FPRs are potential targets for anti-inflammatory therapies. In order to search for potentially novel anti-inflammatory agents, we examined Ganoderma (Lingzhi), a Chinese medicinal herbs known for its anti-inflammatory effects, and found that compound 18 (C18) derived from Ganoderma cochlear could limit the inflammatory response through FPR-related signaling pathways. Further studies showed that C18 could bind to FPR2 and induce conformation change of the receptor that differed from the conformational change induced by the pan-agonist, WKYMVm. C18 inhibited at the receptor level and blocked WKYMVm signaling through FPR2, resulting in reduced superoxide production and compromised cell chemotaxis. These results identified for the first time that a Ganoderma-derived component with inhibitory effects that acts through a G protein-coupled receptor FPR2. Considering its less than optimal IC50 value, further optimization of C18 would be necessary for future applications.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N651 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Recommanded Product: 3682-14-2, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 3682-14-2, Name is 6-Amino-2,3-dihydrophthalazine-1,4-dione, molecular formula is C8H7N3O2

Relative contributions of mitochondria and NADPH oxidase to deoxycorticosterone acetate-salt hypertension in mice

We assessed the relative contribution of the mitochondrial respiratory chain and NADPH (nicotinamide adenine dinucleotide phosphate) oxidase to deoxycorticosterone acetate (DOCA)-salt hypertension in mice. The daily mean arterial pressure was monitored by radiotelemetry in DOCA-salt-treated mice given vehicle or the mitochondrial respiratory chain complex I inhibitor rotenone. This treatment produced remarkable attenuation of DOCA-salt hypertension. Similar results were obtained with other inhibitors of mitochondrial function, including 5-hydroxydecanoate (specific for mitochondrial potassium-ATP channels), benzylguanidine (complexes I and III), and the cell-permeable manganese tetrakis (4-benzoic acid) porphyrin (a mimic of mitochondrial superoxide dismutase). In parallel with the blood pressure-lowering effect of rotenone, the DOCA-salt-induced increases in urinary 8-isoprostane excretion and in reactive oxygen species production of isolated kidney mitochondria were both significantly attenuated. Conversely, the DOCA-salt-induced reduction of urinary nitrate/nitrite excretion was significantly elevated. Following DOCA-salt treatment, mice deficient in NADPH oxidase subunits gp91phox or p47phox exhibited a partial attenuation of the hypertensive response at early but not later time points. Thus, the mitochondrial respiratory chain is a major source of oxidative stress in DOCA-salt hypertension, whereas NADPH oxidase may have a relatively minor role during the early stage of hypertension.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N663 – PubChem

Application of 253-52-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.253-52-1, Name is Phthalazine, molecular formula is C8H6N2. In a Article£¬once mentioned of 253-52-1

Synthesis of aza-naphthindolizinedione derivatives

A series of aza-naphthindolizinedione derivatives, such as indolizinoquinolinedione derivatives, indolizinophthalazinedione derivatives and indolizinoquinoxalinedione derivatives were designed and synthesized. The synthetic pathway was also proposed.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N401 – PubChem

Application of 253-52-1, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 253-52-1, Name is Phthalazine,introducing its new discovery.

Photoredox-Mediated Minisci-type Alkylation of N-Heteroarenes with Alkanes with High Methylene Selectivity

We report a highly efficient and chemoselective Minisci-type alkylation reaction of N-heteroarenes with alkanes under the reagent control of a hypervalent iodine oxidant PFBI-OH. In addition to the high reactivity, PFBI-OH demonstrated a high steric sensitivity for H abstraction of alkanes. This reaction is selective for more sterically accessible secondary C-H bonds over weaker tertiary C-H bonds. High selectivity toward penultimate methylene groups was observed for a wide range of acyclic alkanes.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N255 – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. HPLC of Formula: C8H6N2, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 253-52-1, name is Phthalazine. In an article£¬Which mentioned a new discovery about 253-52-1

New pyrrolo[2,1-a]phthalazine derivatives by one-pot three-component synthesis

The synthesis of the pyrrolo[2,1-a]phthalazine derivatives was performed by an efficient one-pot three-component reaction starting from phthalazine, 2-bromoacetophenones and nonsymmetrical and symmetrical acetylenic dipolarophiles in 1,2-epoxybutane as both reaction medium and HBr scavenger. The structure of the compounds was assigned by IR and NMR spectroscopy. Georg Thieme Verlag Stuttgart New York.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N136 – PubChem

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The synthesis of 6,9-bis[(aminoalkyl)amino] substituted benzo[g]quinoxaline-, benzo[g]quinazoline- and benzo[g]phthalazine-5,10- diones via regiospecific displacements

The synthesis of 6,9-difluoro substituted benzo[g]quinoxaline-5,10-diones (3A), benzo[g]quinazoline-5,10-diones (3B) and benzo[g]phthalazine-5,10- diones (3C) have been accomplished. Treatment of 3A, 3B or 3C with diamines or N-(t-butoxycarbonyl)ethylenediamine led to the corresponding 6,9- bis[(aminoalkyl)amino]-substituted analogues related to 2A, 2B and 2C, respectively. The mono-substituted derivatives 4h and 4i could be isolated from displacements commencing from 3A. A competitive ring-opening of the pyrimidine ring of 2C occurred during the reaction with N,N- dimethylethylenediamine. Removal of the BOC-protecting group from 2Ac led to the hydrochloride salt 2Ab. A novel synthetic pathway to 6,9- dihydroxybenzo[g]phthalazine-5,10-dione (21a) was developed. Conversion of 21a to the ditosylate 21b was readily accomplished. Treatment of 21b with N,N-dimethylethylenediamine or N-(t-butoxycarbonyl)ethylenediamine led to 2Ca and 2Cc, respectively. Removal of the BOC-protecting group from 2Cc with trifluoroacetic acid followed by ion-exchange led to the hydrochloride salt 2Cb. Treatment of ditosylate 21b with N-(t-butoxycarbonyl)ethylenediamine also led to the mono-substituted analogue 25a along with a small amount of the O-S cleavage product 25b. Treatment of 25a with N,N- dimethylethylenediamine led to the unsymmetrically substituted derivative 25c which was converted into the trifluoroacetate salt 25d.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N241 – PubChem

253-52-1, Name is Phthalazine, belongs to phthalazine compound, is a common compound. Recommanded Product: PhthalazineIn an article, once mentioned the new application about 253-52-1.

Synthesis and in vitro evaluation of hydrazinyl phthalazines against malaria parasite, Plasmodium falciparum

In this report, we describe the synthesis of 1-(Phthalazin-4-yl)-hydrazine using bronsted acidic ionic liquids and demonstrate their ability to inhibit asexual stage development of human malaria parasite, Plasmodium falciparum. Through computational studies, we short-listed chemical scaffolds with potential binding affinity to an essential parasite protein, dihydroorotate dehydrogenase (DHODH). Further, these compounds were synthesized in the lab and tested against P. falciparum. Several compounds from our library showed inhibitory activity at low micro-molar concentrations with minimal cytotoxic effects. These results indicate the potential of hydralazine derivatives as reference scaffolds to develop novel antimalarials.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N421 – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Safety of Phthalazine. Introducing a new discovery about 253-52-1, Name is Phthalazine

An Amine Group Transfer Reaction Driven by Aromaticity

A stereoselective domino inverse electron-demand Diels-Alder/amine group transfer reaction catalyzed by a bidentate Lewis acid provides 1-amino-1,2-dihydronaphthalenes, a core structure in many bioactive compounds. A concerted mechanism is proposed based on experimental studies as well as DFT computations demonstrating a new general reactivity scheme. The broad scope of the reaction was evaluated by variation of all three starting compounds, phthalazines, aldehydes, and amines. Scalability was demonstrated by a gram scale reaction without diminished yield.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N23 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: Phthalazine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 253-52-1, Name is Phthalazine, molecular formula is C8H6N2

A new class of luminescent tricarbonyl rhenium(I) complexes containing bridging 1,2-diazine ligands: electrochemical, photophysical, and computational characterization

A novel class of luminescent tricarbonyl rhenium(I) complexes of general formula [Re2(mu-X)2(CO)6(mu-diaz)] (X = halogen and diaz = 1,2-diazine) was prepared by reacting [ReX(CO)5] with 0.5 equiv of diazine (seven different ligands were used). The bridging coordination of the diazine in these dinuclear complexes was confirmed by single-crystal X-ray analysis. Cyclic voltammetry in acetonitrile showed for all the complexes (but the phthalazine derivative) a chemically and electrochemically reversible ligand-centered reduction, as well as a reversible metal-centered bielectronic oxidation. With respect to the prototypical luminescent [ReCl(CO)3(bpy)] complex, the oxidation is more difficult and the reduction easier (about +0.3 V), so that a similar highest occupied molecular orbital-lowest unoccupied molecular orbital gap is observed. All of the complexes exhibit photoluminescence at room temperature in solution, with broad unstructured emission from metal-to-ligand charge-transfer states, at lambda in the range 579-620 nm. Lifetimes (tau = 20-2200 ns) and quantum yields (Phi up to 0.12) dramatically change upon varying the bridging ligand X and the diazine substituents: in particular, quantum yields decrease in the series Cl, Br, and I and in the presence of substituents at the alpha positions of the pyridazine ring. A combined density functional and time-dependent density functional study of the geometry, relative stability, electronic structure, and photophysical properties of all the pyridazine derivatives was performed. The nature of the excited states involved in the electronic absorption spectra was ascertained, and trends in the energy of the highest occupied and lowest unoccupied molecular orbitals upon changing the pyridazine substituents and the bridging halogen ligands were discussed. The observed emission properties of these complexes were shown to be related to a combination of steric and electronic factors affecting their ground-state geometry and their stability.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N130 – PubChem