More research is needed about Phthalazine

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One-pot synthesis of imidazopyridine derivatives

Two highly efficient and general one-pot annulation reactions are described for the synthesis of imidazopyridine derivatives (IPs). The two procedures are complementary to each other: Whereas the first one allows the production of simpler IPs, the second leads to IPs with functionalized imidazole moiety. Both methodologies consist of an activation step, which raises the electrophilicity of the N-heterocyclic starting material (i.e., quaternarization of the N-heterocycle), followed by a cascade reaction involving nucleophilic addition, substitution, rearrangement, and oxidation steps. These methodologies can be used in the synthesis of a library of drug-like molecules. Georg Thieme Verlag Stuttgart.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N334 – PubChem

Archives for Chemistry Experiments of 253-52-1

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Formal Insertion of Imines (or Nitrogen Heteroarenes) and Arynes into the C-Cl Bond of Carbon Tetrachloride

The formal insertion of double and triple bonds into the C-Cl bond of carbon tetrachloride has enabled the full utilization of carbon tetrachloride in chemical synthesis. A range of unactivated imines and electron-deficient nitrogen heteroarenes served as effective sources of C=N bonds to react with arynes and carbon tetrachloride to afford functionalized anilines whose core structures are present in some valuable arthropodicides. Control experiments and DFT calculations suggest the involvement of a trichloromethyl anion intermediate.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N257 – PubChem

Discovery of 253-52-1

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1,3-Dipolar cycloaddition between acetylenic dipolarophiles and sydnone-N-ylides as bis(1,3-dipoles)

1,3-Dipolar cycloaddition reaction of sydnone-N-ylides, as model bis(1,3-dipoles), with acetylenic dipolarophiles in 1,2-epoxybutane under reflux gave exclusively pyrroloazines containing a sydnone moiety that resulted by preferred reaction of the N-ylide 1,3-dipole with the acetylenic dipolarophiles. The assembled sydnone-ylide hybrid structures were generated in situ from N-heteroaromatic bromides. The structure of the new compounds was assigned by IR and NMR spectroscopy and confirmed by X-ray analysis for a representative compound.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N29 – PubChem

Archives for Chemistry Experiments of 253-52-1

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Recyclable Raman chip for detection of trace Mercury ions

Due to enrichment effect of Mercury ions (Hg2+), even if the concentration of Hg2+ is very low, it will do harm to human health. Precise detection of trace Hg2+ is important for environment protection and human health monitoring. In this work, gold nanoparticles (AuNPs) are immobilized on the surface of ITO with aid of inositol-hexaphosphate as linker agent and then 4-pyridinethiol (4-MPy) is decorated to form a 4-MPy/AuNPs/ITO chip. 4-MPy in the chip acts two roles involving the capture agent for Hg2+ and Raman signal reporter. With the adding of Hg2+, the linear increase of SERS response of 4-MPy is in the range from 1.0 ppt to 100 ppb (R2 = 0.9896) and the limit of detection could be down to 1 ppt. The mechanism of the Raman chip was also explored by molecular simulation. It is found that the interaction between Hg2+ and the nitrogen atoms changes the electron distribution of pyridine ring and induces reorientation of the 4-MPy molecules tending to more perpendicular adsorption fashion with respect to AuNPs surface, which leads to enhancement of the intensity of the pyridine breathing vibration peak at 1093 cm?1. The as-prepared SERS sensor chip features excellent stability and reproducibility as well as could be reused. The rapid 4-MPy/AuNPs/ITO-chip-based Raman protocol with capability against interference is competent for monitoring trace Hg2+ in river water samples.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N175 – PubChem

Top Picks: new discover of Phthalazine

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Synthesis, molecular modelling and anticancer evaluation of new pyrrolo[1,2-b]pyridazine and pyrrolo[2,1-a]phthalazine derivatives

Two new series of heterocyclic derivatives with potential anticancer activity, in which a pyrrolo[1,2-b]pyridazine or a pyrrolo[2,1-a]phthalazine moiety was introduced in place of the 3?-hydroxy-4?-methoxyphenyl ring of phenstatin have been synthesised and their structure-activity relationship (SAR) was studied. Fourteen of the new compounds were evaluated for their in vitro cytotoxic activity by National Cancer Institute (NCI) against 60 human tumour cell lines panel. The best five compounds in terms of in vitro growth inhibition were screened in the second stage five dose-response studies, three of them showing a very good antiproliferative activity with GI50<100 nM on several cell lines including colon, ovarian, renal, prostate, brain and breast cancer, melanoma and leukemia. Docking experiments on the biologically active compounds showed a good compatibility with the colchicine binding site of tubulin. A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 253-52-1 Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N348 – PubChem

Brief introduction of 253-52-1

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Effect of commonly used organic solvents on Aldehyde oxidase-mediated Vanillin, Phthalazine and Methotrexate oxidation in human, rat and mouse liver subcellular fractions

1. Aldehyde oxidase (AOX) is a cytosolic molybdoflavoprotein enzyme widely distributed across many tissues. In this study, we report the effect of commonly used organic solvents such as dimethyl sulfoxide (DMSO), acetonitrile (ACN), methanol and ethanol on AOX activity in human, rat and mouse liver S9 fractions using vanillin, phthalazine and methotrexate as probe substrates. 2. Methanol was found to be the most potent solvent in inhibiting vanillic acid and 1-phthalazinone formation in comparison to DMSO, ACN and ethanol across the species tested, except 7-hydroxy methotrexate. 3. Treatment with these solvents at approximate IC50 (% v/v) concentrations showed significant reduction in Clint and Vmax of the probe substrates and also resulted in different effects on Km across the species. 4. Marked differences in the activity and affinity towards AOX were observed with different probe substrates with methotrexate showing least activity and affinity as compared to vanillin and phthalazine. 5. Overall, AOX activity seemed to be more resilient to the presence of organic solvents at higher concentrations in human and rodent species. These results suggest that low concentrations of organic solvents are acceptable for in vitro incubations involving AOX-mediated metabolism.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N64 – PubChem

Extracurricular laboratory:new discovery of 253-52-1

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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.

Silver(i) complexes with quinazoline and phthalazine: Synthesis, structural characterization and evaluation of biological activities

New silver(i) complexes with quinazoline (qz) and phthalazine (phtz), [Ag(NO3)(qz)]n (1) and {[Ag(CH3CN)]2(mu-phtz)2}[BF4]2 (2), have been synthesized and structurally characterized by using different spectroscopic and single-crystal X-ray diffraction techniques. The obtained results revealed that the reaction of AgNO3 with qz at room temperature in a 2 :1 molar ratio led to the formation of the polynuclear complex 1. However, the reaction of AgBF4 with phtz under the same experimental conditions resulted in the formation of the dinuclear complex 2. The solution behaviour and air/light stability of these silver(i) complexes have been investigated. The complexes 1 and 2, along with the silver(i) salts used for their synthesis, were evaluated by in vitro antimicrobial studies against a panel of microbial strains that lead to many skin and soft tissue, respiratory, wound, and nosocomial infections. The obtained results indicate that all tested silver(i) compounds have good antibacterial activity with MIC values in the range from 1.5 to 15.6 mug mL-1 against the investigated strains. On the other hand, their antifungal activity against Candida albicans was moderate. In order to determine the therapeutic potential of 1 and 2, their antiproliferative effect on the normal human lung fibroblast cell line MRC5, hemolytic effect on red blood cells and embryotoxicity on zebrafish (Danio rerio) have also been evaluated.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N390 – PubChem

Some scientific research about 253-52-1

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A Synopsis of the Properties and Applications of Heteroaromatic Rings in Medicinal Chemistry

Five- and six-membered heteroaromatic rings and their benzo-fused homologues are well established as important structural elements in drug design and are well represented in approved drugs. The key properties of these heterocycles that are of?interest to medicinal chemists include lipophilicity, pKa, aromaticity, ionization potential, H-bond acceptor, and H-bond donor (N?H, O?H, C?H) capability, electron withdrawing effects, dipole values, and bond angles. The judicious and productive application of azoles and azines in drug design requires an understanding of the intrinsic physical chemical properties of the individual heterocycles and how these interact with substituents. In this article, the key properties of azole and azine heterocycles are summarized followed by a synopsis of applications where some of these factors play a role in drug?target interactions and/or potency.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N284 – PubChem

Awesome and Easy Science Experiments about Phthalazine

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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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Phthalazine – Wikipedia,
Phthalazine | C8H6N15 – PubChem

A new application about Phthalazine

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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