Archives for Chemistry Experiments of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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A phthalazinone hydroxamic acid derivatives and its preparation method and application (by machine translation)

The invention discloses a has a plurality of poly adenosine diphosphate ribose polymerase (PARP) and/or histone deacetylase (HDAC) inhibitory activity of taitai qin alkone different hydroxy wo acid compounds and preparation method and application thereof. The taitai qin alkone different hydroxy wo acid compounds of the formula I as shown in the structural formula, wherein R1 Is a hydrogen atom or a halogen; R2 Is a hydrogen atom or a halogen; Y is an oxygen atom, methylene or fluorine substituted methylene; Z is or G bond is a chemical bond, methylene, fluoro methylene or double bond. In vitro cell proliferation experiment shows that, as shown in formula I compound well inhibit a variety of tumor cell proliferation. Poly adenosine diphosphate ribose polymerase (PARP) and histone deacetylase (HDAC) inhibition experiment I indicates the type compound is shown to poly adenosine diphosphate ribose polymerase (PARP) and/or histone deacetylase (HDAC) have good inhibitory activity of the compound. (by machine translation)

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Phthalazine – Wikipedia,
Phthalazine | C8H6N746 – PubChem

Properties and Exciting Facts About Phthalazine

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Exploration of 1,2-phenylenediboronic esters as potential bidentate catalysts for organic synthesis

Recently, we described the first inverse electron demand Diels-Alder reaction of 1,2-diazene catalyzed by a bidentate Lewis acid. Herein we investigate 1,2-phenylenediboronic esters as potential catalysts for this transformation offering higher stability and easier handling than the currently used boranthracene derivatives. Different 1,2-phenylenediboronic esters were prepared and their ability to form bidentate coordination complexes with phthalazine was analyzed. Although a 1:1 complex was observed, X-ray analysis revealed binding only in a monodentate fashion.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N50 – PubChem

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of 6-Amino-2,3-dihydrophthalazine-1,4-dione, 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

Oregonin reduces lipid accumulation and proinflammatory responses in primary human macrophages

Inflammation in the vascular wall is important for the development of atherosclerosis. We have previously shown that inflammatory macrophages are more abundant in human atherosclerotic lesions than in healthy arteries. Activated macrophages produce reactive oxygen species (ROS) that promote local inflammation in atherosclerotic lesions. Here, we investigated the role of oregonin, a diarylheptanoid, on proinflammatory responses in primary human macrophages and found that oregonin decreased cellular lipid accumulation and proinflammatory cytokine secretion. We also found that oregonin decreased ROS production in macrophages. Additionally, we observed that treatment of lipopolysaccharide-exposed macrophages with oregonin significantly induced the expression of antioxidant-related genes, including Heme oxygenase-1 and NADPH dehydrogenase quinone 1. In summary, we have shown that oregonin reduces lipid accumulation, inflammation and ROS production in primary human macrophages, indicating that oregonin has anti-inflammatory bioactivities.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N600 – PubChem

Awesome Chemistry Experiments For Phthalazine

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Quantitative study of the structural requirements of phthalazine/quinazoline derivatives for interaction with human liver aldehyde oxidase

Aldehyde oxidase is a molybdenum-containing enzyme distributed throughout the animal kingdom. Although this enzyme is capable of metabolizing a wide range of aldehydes and N-heterocyclic compounds, there is no reported detailed study of physicochemical requirements of the enzyme-substrate interactions. The aim of this study, therefore, was to investigate quantitatively the relationships between the kinetic constants of aldehyde oxidase-catalyzed oxidation of some phthalazine and quinazoline derivatives (as substrates) and their structural parameters. Multiple regression and stepwise regression analyses showed that polarity of phthalazines (expressed as dipole moment mu, cohesive energy density deltaT and an indicator variable for hydrogen-bond acceptor ability of R1 substituent, HBA) had a negative effect on the enzyme activity (leading to the reduction of Vmax and increase of Km). Electron withdrawing substituents in the quinazoline series are favorable for interaction with the enzyme. This finding and also the relationships of 1/Km of phthalazines with the energy of the lowest unoccupied molecular orbital and log Vmax/logKm of phthalazines with degree of bonding of the two nitrogen atoms in the molecules are consistent with the mechanism of action. The reaction involves a nucleophilic attack on an electron-deficient sp2-hybridized carbon atom and formation of an epoxide intermediate following the disruption of the aromatic structure.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N163 – PubChem

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Phytochemical Profile, Pharmacological Attributes and Medicinal Properties of Convolvulus prostratus ? A Cognitive Enhancer Herb for the Management of Neurodegenerative Etiologies

Convolvulus prostratus Forssk., a nootropic herb used in traditional medicinal systems, is also frequently known by its taxonomic synonym Convolvulus pluricaulis. In Indian medicinal system ? Ayurveda ? it is named as Shankhpushpi. According to the ancient literature, this herb has been attributed with several therapeutic properties, such as anxiolytic, neuroprotective, antioxidant, analgesic, immunomodulatory, antimicrobial, antidiabetic and cardioprotective activities. This medicinal herb has been reported to contain many bioactive phytoconstituents, such as, alkaloid (convolamine), flavonoid (kaempferol) and phenolics (scopoletin, beta-sitosterol and ceryl alcohol), that have been ascribed to the observed medicinal properties. Several research teams across the globe have highlighted the neuro-pharmacological profile of C. prostratus, wherein, the neuroprotective, nootropic and neuro-modulatory roles have been described. Besides, role of C. prostratus extracts in neurodegeneration has been well demonstrated. Despite of such elaborative preclinical pharmacological profile, detailed clinical investigations and mechanistic mode-of-action studies of this important herb are yet to be executed. The present review is attempted to showcase the phytochemical profile, pharmacological attributes and medicinal information of C. prostratus; with comprehensive research gap analysis. It is hoped that the scientific update on the ethnomedicinal aspects of this herb would thrive research propagation and development of the CNS phytopharmaceuticals, originated from C. prostratus.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N53 – PubChem

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Recent advances in the synthesis of biologically active cinnoline, phthalazine and quinoxaline derivatives

In the recent decades, N-heterocycles are widely used as versatile scaffolds for the development of biologically active compounds and considered as one of the privileged structures. Among the various N-heterocycles, benzodiazines, a series of bicyclic heterocycles in which benzene rings are fused with 6-membered heterocycles containing two nitrogens are especially interesting, due to their structural conciseness and usefulness as synthetic intermediates, and suitable physicochemical properties as potential drug candidates and chemical probes. For this reason, a series of synthetic methodologies for benzodiazines has been developed and generally used in organic and medicinal chemistry fields. Interestingly, synthesis of quinazoline, a kind of benzodiazine in which benzene is fused with pyrimidine, has been extensively reviewed, while cinnoline, phthalazine and quinoxaline, benzene fused with pyridazine or pyrazine, have been relatively less investigated. In this review, recent advances in the synthesis of biologically active benzodiazines, benzene ring-fused 6-membered heterocycles with two nitrogen atoms, cinnoline, phthalazine and quinoxaline, will be addressed. In each section, biological activities of various benzodiazines, recently served as novel scaffolds for drug discovery, are briefly summarized for comprehensive understanding of biological and medicinal significance in advance. Moreover, intensive investigation of the synthetic approaches to various benzodiazines such as cinnoline, phthalazine and quinoxaline is followed. It would hopefully be helpful for the readers who have interests in developing novel drug candidates and related useful chemical probes.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N178 – PubChem

New explortion of Phthalazine

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Direct Arylation of Unactivated Alkanes with Heteroarenes by Visible-Light Catalysis

The functionalization of aliphatic C-H bonds is both a major challenge and a desirable goal in organic synthesis. Here, we describe the successful arylation of unactivated alkanes with heteroarenes by using iridium polypyridyl complexes as the photocatalyst and persulfate as the HAT catalyst precursor under visible-light irradiation. This reaction features good functional group tolerance and broad scope with regard to both alkane and heteroarene substrates (37 examples), which allows direct access to alkyl-substituted N-heteroarenes, a key structural motif in natural products and bioactive molecules.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N194 – PubChem

Final Thoughts on Chemistry for 6-Amino-2,3-dihydrophthalazine-1,4-dione

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Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of 6-Amino-2,3-dihydrophthalazine-1,4-dione, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 3682-14-2

Blastomyces dermatitidis serine protease dipeptidyl peptidase IVA (DppIVA) cleaves ELR+CXC chemokines altering their effects on neutrophils

Blastomycosis elicits a pyogranulomatous inflammatory response that involves a prominent recruitment of neutrophils to the site of infection. Although neutrophils are efficiently recruited to the site of infection, this event is paradoxically coupled with the host’s inability to control infection by Blastomyces dermatitidis, the causative agent. The mechanisms underlying this characteristic pyogranulomatous response and inability of neutrophils to kill the yeast are poorly understood. We recently reported that the fungal protease dipeptidyl peptidase IVA (DppIVA) promotes B.?dermatitidis virulence by cleaving a dipeptide from the N-terminus of C?C chemokines and granulocyte/macrophage-colony stimulating factor, thereby inactivating them. Herein, we present evidence that DppIVA can also truncate the N-terminus of members of the ELR+CXC chemokine family, which are known to modulate neutrophil function. We show that the DppIVA cleaved form of human (h) CXCL-2, for example, hCXCL-2 (3-73), is a more potent neutrophil chemoattractant than its intact counterpart, but hCXCL-2 (3-73) is conversely impaired in its ability to prime the reactive oxygen species response of neutrophils. Thus, DppIVA action on ELR+CXC chemokines may promote the pyogranulomatous response that is typical of blastomycosis, while also explaining the inability of neutrophils to control infection.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N599 – PubChem

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Continuous amination of aryl/heteroaryl halides using aqueous ammonia in a Teflon AF-2400 tube-in-tube micro-flow reactor

The annual production of primary (hetero)arylamines has exceeded 6 million tons and has been extensively employed in the pharmaceutical, agrochemical, and materials industries. Catalyst-free and protecting group-free nucleophilic amination using ammonia represents a green and atom-economical method. However, due to the innate reactivity, chemical compatibility issue and the safety hazardous properties of ammonia gas, such transformation is still underused. By implementing a gas-permeable Teflon AF-2400 tube-in-tube system, diffusion of NH3 from aqueous ammonia to a reaction mixture for amination can be achieved in a continuous flow fashion. In this communication, we herein report the use of aqueous ammonia as the NH3 source in the amination of heteroaryl chorides to generate primary heteroaryl amines, providing a protocol that is green, economical and safe.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N487 – PubChem

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Monoazole ligand platinum analogs

Disclosed herein are novel platinum-based analogs with a single substituted azole ligand: RN=NR7, wherein the RN=NR7 functional group is covalently bonded to the platinum through nitrogen of NR7. The analogs also have nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA, and one or more leaving groups which can be displaced by water, hydroxide ions or other nucleophiles, which is thought to form active species in vivo, and then, form cross-linked complexes between nucleic acid strands, principally between purines in DNA (or RNA), i.e., at the Guanine or Adenine bases, thereof. These platinum analogs may also be more easily transported into tumor cells, due to their increased lipophilicity and are likely to be useful as anti-neoplastic agents, and in modulating or interfering with the synthesis or replication or transcription of DNA or translation or function of RNA in vitro or in vivo, as they are potentially capable of forming a platinum coordinate complex with an intact or nascent DNA or RNA and thereby interfering with cellular synthesis, transcription or replication of nucleic acid polynucleotides.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N15 – PubChem