Extracurricular laboratory:new discovery of 4-(4-Chlorobenzyl)phthalazin-1(2H)-one

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Anti-Trypanosoma activity of some natural stilbenoids and synthetic related heterocyclic compounds

We report the anti-Chagasic activity of the natural dihydrostilbenoid isonotholaenic acid and several simple derivatives, as well as that of some representative compounds of related synthetic series, with basic structures of benzalphthalides, dihydrostilbamides, isoindoles, phthalazin-1-ones, imidazo[2,1-a]isoindoles and pyrimido[2,1-a]isoindoles. The evaluation was performed in vitro on cultures of epimastigote and trypomastigote forms of Trypanosoma cruzi. Some of the tested compounds resulted to be as potent as benznidazole (epimastigotes), and others were shown to be more active than gentian violet (trypomastigotes), used as reference drugs.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N729 – PubChem

Discovery of Phthalazine

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Review of the methods for determination of reactive oxygen species and suggestion for their application in advanced oxidation induced by dielectric barrier discharges

Advanced oxidation processes (AOPs) particularly non-thermal plasmas based on electrical discharges have been widely investigated for water and wastewater treatment. Dielectric barrier discharges (DBDs) generate large amounts of selective and non-selective reactive oxygen species (ROS) such as ozone, hydrogen peroxide, atomic oxygen, superoxide molecular anions and hydroxyl radicals, having been proved to be efficient for water decontamination among various forms of electrical discharge systems. The detection and quantification methods of these oxygen species in non-thermal plasmas have been reviewed. However, their application in dielectric barrier discharge has not been well studied. It is therefore imperative to summarise the various detection and quantification methods for oxygen-based species determination in AOPs, aqueous systems and non-thermal plasma processes. Thereafter, reviewed methods are suggested for the determination of ROS in DBD configurations to understand the consumption trend of these oxidants during treatment of water effluents and to evaluate the performance of the treatment reactor configuration towards the degradation of targeted pollutants.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N282 – PubChem

Archives for Chemistry Experiments of 2-(3-(4-Bromo-2-fluorobenzyl)-4-oxo-3,4-dihydrophthalazin-1-yl)acetic acid

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Synthesis, activity, and molecular modeling of new 2,4-dioxo-5- (naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues as potent aldose reductase inhibitors

A series of 2,4-dioxo-5-(2-naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues have been prepared as aldose reductase inhibitors. In vitro inhibitory activities of bovine lens aldose reductase were determined by a conventional method. 1-Naphthyl-substituted derivafives of the 2-thioxo series were the more potent inhibitors (IC50 ? 10 nM) with similar activity to that of Epalrestat. Structural analysis, especially by X-ray crystallography of two selected compounds, and molecular modeling comparisons with Zopolrestat were performed. These results provide explanations of the good activity of the inhibitor, the preference for 1-naphthyl-substituted compounds, and the nature of molecular interactions in these systems.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N862 – PubChem

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Synthesis and Properties of (Phthalocyaninato)ruthenium(II) with Bisaxially Coordinated Azanaphthalenes

(Phthalocyaninato)ruthenium(II) (PcRu) reacts with different azanaphthalenes such as quinoxaline, 2-methylquinoxaline, quinazoline, phthalazine, quinoline, pyrido<2,3-b>pyrazine, pteridine, isoquinoline and 1,5-naphthyridine to form the corresponding bisaxially coordinated PcRuL2 complexes 1 -9.The IR, 1H-NMR, UV/Vis, TG/DTA, and FD-MS data are discussed in detail for all the complexes prepared. Key Words : Phthalocyanine / Ruthenium complexes / Azanaphthalenes

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Phthalazine – Wikipedia,
Phthalazine | C8H6N179 – PubChem

Discovery of Phthalazine

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Bridging ligands comprising two or more di-2-pyridylmethyl or amine arms: Alternatives to 2,2′-bipyridyl-containing bridging ligands

Bridging ligands incorporating 2,2′-bipyridine as a chelating component have been utilised for several decades and are widely employed in coordination chemistry, supramolecular chemistry and materials synthesis. Such ligands form stable 5-membered chelate rings upon coordination to a metal. Two related chelating units, di-2-pyridylamine and di-2-pyridylmethane, which form 6-membered chelate rings when coordinated to a metal, have been studied far less as components of bridging ligands but have recently garnered significant levels of attention. Of around 140 reports on the incorporation of these moieties into bridging ligands some 75% have been published in the last 15 years. This review covers the synthesis of bridging ligands containing di-2-pyridylamine and di-2-pyridylmethane chelating moieties, and a survey of their coordination and supramolecular chemistry. Applications of the resulting systems as structural and functional models of enzyme active sites, and spin-crossover materials, and for investigations into anion-pi interactions are covered.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N426 – PubChem

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PARP-1-targeted radiotherapy in mouse models of glioblastoma

The DNA repair enzyme poly(ADP-ribose) polymerase 1 (PARP-1) is overexpressed in glioblastoma, with overall low expression in healthy brain tissue. Paired with the availability of specific small molecule inhibitors, PARP-1 is a near-ideal target to develop novel radiotherapeutics to induce DNA damage and apoptosis in cancer cells, while sparing healthy brain tissue. Methods: We synthesized an 131I-labeled PARP-1 therapeutic and investigated its pharmacology in vitro and in vivo. A subcutaneous tumor model was used to quantify retention times and therapeutic efficacy. A potential clinical scenario, intratumoral convection-enhanced delivery, was mimicked using an orthotopic glioblastoma model combined with an implanted osmotic pump system to study local administration of 131I-PARPi (PARPi is PARP inhibitor). Results: 131IPARPi is a 1(2H)-phthalazinone, similar in structure to the Food and Drug Administration-approved PARP inhibitor AZD-2281. In vitro studies have shown that 131I-PARPi and AZD-2281 share similar pharmacologic profiles. 131I-PARPi delivered 134.1 cGy/ MBq intratumoral injected activity. Doses to nontarget tissues, including liver and kidney, were significantly lower. Radiation damage and cell death in treated tumors were shown by p53 activation in U87-MG cells transfected with a p53-bioluminescent reporter. Treated mice showed significantly longer survival than mice receiving vehicle (29 vs. 22 d, P , 0.005) in a subcutaneous model. Convection-enhanced delivery demonstrated efficient retention of 131I-PARPi in orthotopic brain tumors, while quickly clearing from healthy brain tissue. Conclusion: Our results demonstrate 131IPARPi’s high potential as a therapeutic and highlight PARP’s relevance as a target for radionuclide therapy. Radiation plays an integral role in brain tumor therapy, and radiolabeled PARP therapeutics could ultimately lead to improvements in the standard of care.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N821 – PubChem

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One pot, four-component synthesis 2-amino-6-(1,4-dioxo-3,4-dihydrophthalazin-2(1H)-yl)-4-aryl-4H-pyran-3,5-dicarbonitriles in an ionic liquid

[DBUH][OAc] (1,8-diazabicyclo[5.4.0]-undec-7-en-8-ium acetate) mediated, green synthesis of 2-amino-6-(1,4-dioxo-3,4-dihydrophthalazin-2(1H)-yl)-4-aryl-4H-pyran-3,5-dicarbonitriles have been synthesized by condensing diethyl phthalate, ethyl cyanohydrazide, benzaldehydes and malononitrile in [DBUH][OAc] medium, at 60-65 C for 2 h. Particularly valuable features of this method include high yield, broad substrate scope, shorter reaction times and straightforward procedure.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N265 – PubChem

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Photoredox-mediated remote C(sp3)-H heteroarylation of free alcohols

We report an efficient and economical method for remote delta C(sp3)-H heteroarylation of free aliphatic alcohols using a hypervalent iodine PFBI-OH oxidant under photoredox catalysis. The reaction sequence involves in situ alcoholysis of PFBI-OH with alcohol, generation of an alkoxy radical intermediate by SET reduction, 1,5-HAT, and Minisci-type C-C bond formation. This method uses a slight excess of alcohols, can facilitate reaction at delta methyl and methylene positions, and has been successfully applied to modification of complex drug molecules.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N256 – PubChem

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Quinazoline pharmacophore in therapeutic medicine

This present study comprehensively expatiates the functionalized utilization of quinazoline scaffolds in drug development and furnishes latest updates in pharmacological appositeness of its derivatives in order to reveal novel pathways for therapeutic targets. It traverses numerous biological potentials of quinazoline in the contemporary time to allow researchers? unhindered access to the beneficial role of quinazoline in fighting infectious diseases for future drug discovery. This work provides broad overview of medicinal survey of quinazoline chemistry valuable in the discovery of more efficient clinical trials and to summarize the most promising molecular targets for drug design.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N27 – PubChem

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Molecular Oxygen-Mediated Minisci-Type Radical Alkylation of Heteroarenes with Boronic Acids

The carbon-carbon bond formation via autoxidation of organoboronic acid using 1 atm of O2 is achieved in a simple, clean, and green fashion. The approach allows a technically facile and environmentally benign access to structurally diverse heteroaromatics with medicinally privileged scaffolds. The strategy also displays its practicality and sustainability in the resynthesis of marketed drugs Crestor and pyrimethamine.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N509 – PubChem