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Amino-substituted tetrahydro pyrido pyrimidine compound or its salts and its preparation method and application (by machine translation)

The invention discloses an amino substituted tetrahydro pyrido pyrimidine compound or its salts and its preparation method and application. The compound or its salts having the following general structure or , Wherein R1 , R2 Is C1 – 5 alkyl or amino; R3 With a N 5 – 6 […] members of the heterocyclic radical, the heterocyclic substituent is a nitrogen-containing, containing alkyl-substituted nitrogen or oxygen-containing heterocyclic group. The compound or its pharmaceutically acceptable salt has potent PARP1 inhibitory activity, can be used for treating diseases or cancer drug used for prevention and/or treating PARP1 related diseases. (by machine translation)

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N772 – PubChem

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Potent inhibition of human liver aldehyde oxidase by raloxifene

The selective estrogen receptor modulator, raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta 1?(5?)-iminium ion, with Ki values of 0.87 to 1.4 nM. Inhibition was not time-dependent. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM. However, raloxifene had only small effects on xanthine oxidase, an enzyme related to aldehyde oxidase. In addition, several other compounds of the same therapeutic class as raloxifene were examined for their potential to inhibit aldehyde oxidase. However, none were as potent as raloxifene, since IC50 values were orders of magnitude higher and ranged from 0.29 to 57 muM. In an examination of analogs of raloxifene, it was shown that the bisphenol structure with a hydrophobic group on the 3-position of the benzthiophene ring system was the most important element that imparts inhibitory potency. The relevance of these data to the mechanistic understanding of aldehyde oxidase catalysis, as well as to the potential for raloxifene to cause drug interactions with agents for which aldehyde oxidase-mediated metabolism is important, such as zaleplon or famciclovir, is discussed.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N323 – PubChem

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Validated LC method for the estimation of hydralazine hydrochloride in pharmaceutical dosage forms

A simple and specific liquid chromatographic method has been developed and validated for the estimation of hydralazine hydrochloride injection using HPLC. All the analytical parameters were determined as per ICH Q2B guidelines. Good chromatographic separation was achieved with Inertsil L10 packed column (4.6 mm ¡Á 150 mm, 5 mum particle size) at a wavelength of 230 nm using phosphate buffer and acetonitrile (77: 23) as mobile phase with a flow rate of 1.0 ml/ min. The resolution, between phthalazine and hydralazine hydrochloride peak is not less than 4.0. From the statistical treatment of the linearity data of Hydralazine HCl, it is clear that the response of Hydralazine HCl is linear between 50% to 150% level. The correlation coefficient is greater than 0.998. In addition, the analysis of residuals shows that the values are randomly scattered around zero, which fits, and well within the linear model. The developed method showed good linearity, reproducibility, precision and can be suitably applied for the routine quality control analysis in the estimation of commercial formulations.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N219 – PubChem

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Long-lasting chemiluminescence hydrogels made in situ

Alginate, a natural polysaccharide, can form gels with divalent cations under mild conditions. In this paper, homogeneous, injectable chemiluminescence hydrogels were prepared in situ for the first time. The raw materials contained alginate, calcium ion source (CaCO3), D-glucono-delta-lactone (GDL), chemiluminescence reagent (isoluminol), and catalyst (Co2+). When H2O2 was added, the hydrogels would give blue light which was visible to naked eyes. And, the light emission could last for over 10 h due to the slow-diffusion-controlled chemical reaction. In addition, the as-prepared CL hydrogels had a good response capacity to H2O2.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N659 – PubChem

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Containing the phthalazine -1 (2 H) – one structure of PARP – 1 and PI3K double-target inhibitors (by machine translation)

The invention relates to the field of pharmaceutical chemistry, in particular relates to a containing phthalazine – 1 (2 H) – one and triazine or pyrimidine structure of PARP – 1 and PI3K double-target inhibitor (I), processes for their preparation, and pharmaceutical compositions containing these compounds. The pharmacodynamics experiment proves that the compounds of this invention have anti-tumor efficacy. (by machine translation)

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N775 – PubChem

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Second Harmonic Generation at a Silver Electrode in the Presence of Phthalazine

Second harmonic generation (SHG) and surface-enhanced Raman Scattering (SERS) are used to examine the phthalazine-silver electrode interface over a wide potential range.The SHG signal is found to exhibit hysteresis negative of the potential of zero charge, in contrast to SERS, which shows the exported irreversible degradation of signal.Hysteresis in the second harmonic signal is likely the results of anion-mediated reorientation of phthalazine.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N462 – PubChem

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Elimination Reactions of Hydrazonium Salts: Experimental and Theoretical Evidence for a Large Stereoelectronic Effect of Nitrogen

Elimination of trimethylamine from hydrazonium salts (8, R = Me) is promoted by base (methoxide ion in methanol).The mechanism is characterized as E2 as shown by substituent effects (rho = +2.57), Broensted coefficients, a primary kinetic isotope effect (kH/kD = 2.10), and solvent effects.Variation in the leaving group (8, R = arylmethyl) shows that N-N bond cleavage is less well advanced in the transition state than C-H bond breaking.The elimination to give the nitrile is syn-periplanar and, using the phthalazinium salt 4 as a model for the anti elimination, an anti/syn ratio of ca. 102 is found.The reactions have been modelled using ab initio methods with the transition structures located at the HF/3-21G level and relative energies computed using the MP2/6-31G* method.Using both H2O and NH3 as model bases to induce elimination on +, the calculated energy for anti elimination is lower (in the range 11-13 kcal mol-1) than that for syn elimination.The implications of the results for the ease of formation of nitriles from aldehydes via the hydrazonium salt route are discussed.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N318 – PubChem

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Syntheses, structures, thermal and luminescent properties of cadmium(II) complexes based on quinazoline and phthalazine

Six cadmium(II) compounds [Cd(Qnz)2(SCN)2] n (1), [Cd(Qnz)2(dca)2]n (2), [Cd(Qnz)2(N3)2]}n (3), [Cd 2(mu-SCN-kappa2N:S)2(SCN) 2(Ptz)4(H2O)2] (4), [Cd(Ptz) 2(dca)2]n (5) and [Cd(Ptz)(MeOH)(N 3)2]n (6) were successfully synthesized and characterized by single-crystal diffraction. Additionally, the samples were characterized by powder X-ray diffraction (PXRD), thermal analysis and IR spectroscopy. The fluorescence properties of 1, 2, 3, 5 and 6 were studied in solid state, while emission spectrum of 4 was recorded in methanolic solution. All they were compared with the fluorescence properties of the free ligands. Additionally, the electronic spectrum of 4 was investigated at the TDDFT level employing B3LYP functional in combination with LANL2DZ.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N272 – PubChem

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Anti- Angiogenic therapy: Strategies to develop potent VEGFR-2 tyrosine kinase inhibitors and future prospect

Tumor angiogenesis has always been a major gap for effective cancer therapy. Interruption of aberrant angiogenesis by specific inhibitors targeting receptor tyrosine kinases (RTKS) has been of great interests to medicinal chemists. Among the factors that are involved in tumor angiogenesis, vascular endothelial growth factor receptor-2 (VEGFR-2) is validated as the most closely related factor which can drive angiogenesis through binding with its natural ligand VEGF. The well-validated VEGF-driven VEGFR-2 signaling pathway can stimulate many endothelial responses, including increasing vessel permeability and enhancing endothelial cell proliferation, migration and differentiation. Consequently, circumventing angiogenesis by VEGFR-2 inhibitors represents a promising strategy for counteracting various VEGFR-2-mediated disorders as well as drug resistance. Over the past decades, a considerable number of novel small molecular VEGFR-2 inhibitors have been exploited with diverse chemical scaffolds. Especially, recent frequently launched inhibitors have declared their research values and therapeutic potentials in oncology. Still, the antiangiogenesis based treatment remains an ongoing challenge. In this review, a comprehensive retrospective of newly emerged VEGFR-2 inhibitors have been summarized, with the emphasis on the structure- Activity relationship (SAR) investigation, and also binding patterns of representative inhibitors with biotargets. On the basis of all of this information, varied strategies for developing potent VEGFR-2 inhibitors and the future prospect of the clinical application of antiangiogenic inhibitors are discussed hereby.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N405 – PubChem

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Intersystem Crossing of Radical Pair in Solvent Cage. External Heavy Atom Effect on Dual Photoreactions of Phthalazine

The effects of the temperature, initial concentration, and chemical quenchers on dual photoreactions of phthalazine were investigated.The results give further supporting evidence for a previously proposed reaction mechanism, i.e., phthalazine in the lowest excited singlet and triplet states affords singlet and triplet radical pairs, respectively, in the initial hydrogen abstraction process from 2-propanol.The singlet radical pair gives a reduction product in a solvent cage, whereas the radicals produced in the triplet state escape from the solvent cage, causing dimerization.On the basis of the reaction mechanism of dual photoreactions, external heavy-atom effects on the radical pairs within a solvent cage have been studied.The results indicate that heavy-atom perturbations bring about an enhancement of the intersystem crossing efficiency from the triplet-state radical pair to the singlet one, including a spin inversion of the radical pair in the solvent cage, rather than S1 -> T1 intersystem crossing induced within a single molecule of phthalazine.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N201 – PubChem