More research is needed about 253-52-1

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Sonogashira Reaction: Synthesis of Novel Derivatives of 3-Aryl-Substituted 6-Chloroimidazo[2, 1-a]phthalazines Catalyzed by Pd-Cu in Water

The reaction of 1-chloro-4-propargylaminophthalazine with various aryl halides catalyzed by Pd?Cu in the presence of potassium carbonate, as the base, in water leads to the one-pot formation of new derivatives of 3-aryl-substituted-6-chloroimidazo-[2, 1-a]phthalazines in moderate-to-good yields. Their structures are confirmed by IR and NMR spectra as well as elemental analyses. All the compounds prepared are screened in vitro for their anti-bacterial activities. The preliminary results indicate that some target compounds exhibit promising anti-bacterial potency.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N51 – PubChem

New explortion of Phthalazine

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Reaction of six-membered azaaromatics with allyltributyltin

Pyridazines were reacted with allyltributyltin in the presence of chloroformate to give 1-alkoxycarbonyl-6-allyl and 1-alkoxycarbonyl-4-allyldihydropyridazines as major and minor products, respectively. The reaction system was applied to other diazines and pyrimidine and pyrazine were shown to afford diallyltetrahydroadducts. Benzodiazines also gave allylation products in good yields. The reaction seems to be applicable to most six-membered azaaromatics.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N206 – PubChem

Properties and Exciting Facts About Phthalazine

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Evaluation of new dihydrophthalazine-appended 2,4-diaminopyrimidines against Bacillus anthracis: Improved syntheses using a new pincer complex

The synthesis and evaluation of ten new dihydrophthalazine-appended 2,4-diaminopyrimidines as potential drugs to treat Bacillus anthracis is reported. An improved synthesis utilizing a new pincer catalyst, dichlorobis[1-(dicyclohexylphosphanyl)-piperidine]palladium(II), allows the final Heck coupling to be performed at 90C using triethylamine as the base. These milder conditions have been used to achieve improved yields for new and previously reported substrates with functional groups that degrade or react at the normal 140C reaction temperature. An analytical protocol for separating the S and R enantiomers of two of the most active compounds is also disclosed. Finally, the X-ray structure for the most active enantiomer of the lead compound, (S)-RAB1, is given.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N304 – PubChem

Archives for Chemistry Experiments of 763114-26-7

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Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 763114-26-7

Synthesis, preliminarily biological evaluation and molecular docking study of new Olaparib analogues as multifunctional PARP-1 and cholinesterase inhibitors

A series of new Olaparib derivatives was designed and synthesized, and their inhibitory activities against poly (ADP-ribose) polymerases-1 (PARP-1) enzyme and cancer cell line MDA-MB-436 in vitro were evaluated. The results showed that compound 5l exhibited the most potent inhibitory effects on PARP-1 enzyme (16.10 ¡À 1.25 nM) and MDA-MB-436 cancer cell (11.62 ¡À 2.15 muM), which was close to that of Olaparib. As a PARP-1 inhibitor had been reported to be viable to neuroprotection, in order to search for new multitarget-directed ligands (MTDLs) for the treatment of Alzheimer?s disease (AD), the inhibitory activities of the synthesized compounds against the enzymes AChE (from electric eel) and BChE (from equine serum) were also tested. Compound 5l displayed moderate BChE inhibitory activity (9.16 ¡À 0.91 muM) which was stronger than neostigmine (12.01 ¡À 0.45 muM) and exhibited selectivity for BChE over AChE to some degree. Molecular docking studies indicated that 5l could bind simultaneously to the catalytic active of PARP-1, but it could not interact well with huBChE. For pursuit of PARP-1 and BChE dual-targeted inhibitors against AD, small and flexible non-polar groups introduced to the compound seemed to be conducive to improving its inhibitory potency on huBChE, while keeping phthalazine-1-one moiety unchanged which was mainly responsible for PARP-1 inhibitory activity. Our research gave a clue to search for new agents based on AChE and PARP-1 dual-inhibited activities to treat Alzheimer?s disease.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N789 – PubChem

More research is needed about 2-Fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoic acid

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RADIOLABELLED COMPOUND

The present invention relates to radiolabelled olaparib and in particular [ 18 F]olaparib, a process for producing radiolabelled olaparib, and uses of radiolabelled olaparib in medical imaging.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N742 – PubChem

New explortion of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

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Reference of 763111-47-3, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, molecular formula is C20H19FN4O2. In a Patent£¬once mentioned of 763111-47-3

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 | C8H6N805 – PubChem

Properties and Exciting Facts About Phthalazine

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FACILE RADICAL DECARBOXYLATIVE ALKYLATION OF HETEROAROMATIC BASES USING CARBOXYLIC ACIDS AND TRIVALENT IODINE COMPOUNDS

Many kinds of heteroaromatic bases were easily alkylated by the reaction of carboxylic acids with benzene or pentafluorobenzene via radical decarboxylative pathways.This system was further applied to the reaction with tetrahydrofurylcarboxylic acid, 1-(2,3,5-tri-O-benzyl)-D-ribofuranosylacetic acid, and 1-(2,3,5-tri-O-benzyl)-D-ribofuranosylcarboxylic acid for the model synthesis of C-nucleosides.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N449 – PubChem

Awesome Chemistry Experiments For 253-52-1

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Novel triazolophthalazine-hydrazone hybrids as potential PCAF inhibitors: Design, synthesis, in vitro anticancer evaluation, apoptosis, and molecular docking studies

Three novel series of triazolophthalazine derivatives bearing hydrazone moiety were designed, synthesized, and evaluated for their anticancer activity against four human cancer cell lines by MTT assay. Six derivatives demonstrated comparable activity with Doxorubicin reference drug against the selected cancer cells. Especially, compound 16 showed the most potent activity with IC50 values of 5.70, 8.04, 11.15, and 4.25, muM against HePG2, MCF-7, PC3, and HCT-116 respectively. Also, compound 26 exhibited comparable inhibitory effect with that of Doxorubicin against the selected cancer cell lines with IC50 values of 6.45, 8.63, 12.28, and 7.03 muM against HePG2, MCF-7, PC3, and HCT-116 respectively. Investigation of the apoptotic activity of the two most active compounds revealed that compounds 16 and 26 could induce both the early and the late apoptosis of HePG2. Further mechanistic study of the HePG2 cell cycle confirmed the spectacular cytotoxic and apoptotic effects of both compounds. Compounds 16 and 26 showed a pronounced increase in cells in G2/M and Pre G1 phases with a concomitant reduction of cells in G0-G1 and S phases. A follow up enzymatic assay indicated that these two compounds have comparable activities with that of bromosporine as PCAF inhibitors with IC50 values of 8.13 and 5.31 muM respectively. Moreover, molecular docking study for all the synthesized compounds was performed to predict their binding affinities toward the active site of histone acetyltransferase GCN5. Results of molecular docking were strongly correlated with that of the cytotoxicity study.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N18 – PubChem

More research is needed about 3682-14-2

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Application of 3682-14-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.3682-14-2, Name is 6-Amino-2,3-dihydrophthalazine-1,4-dione, molecular formula is C8H7N3O2. In a Article£¬once mentioned of 3682-14-2

Hydrazide derivatives of luminol for chemiluminescence-labelling of macromolecules

A series of chemiluminescent compounds containing a hydrazide group as a nucleophilic functional group has been synthesized. The syntheses were started from chemiluminescent luminol and isoluminol. The linker moiety was easily introduced onto non-nucleophilic exocyclic amino groups of luminol and isoluminol by gentle heating with cyclic acid anhydrides such as glutaric anhydride. The resulting carboxy group was converted to hydrazide by a simple condensation reaction using carbodiimide. Although majority of the synthesized compounds did not emit strong light, a sufficient chemiluminescence intensity was obtained from luminolamido- C2-hydrazide (L2H) comprising of luminol scaffold with a dimethylene linker. The ability of L2H to form a covalent bond with a macromolecule was further investigated by incubation with oxidized horseradish peroxidase. The analysis on matrix assisted laser desorption/ionization-time of flight (MALDI-TOF) MS revealed that the coupling efficiency of L2H was similar to that of commercially available labelling reagent having a hydrazide group. These results suggested that L2H, the luminol hydrazide containing a dimethylene linker, could be useful for the labelling of macromolecules in the sensitive bioassay such as chemiluminescence immunoassay.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N634 – PubChem

Brief introduction of 6-Amino-2,3-dihydrophthalazine-1,4-dione

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Electric Literature of 3682-14-2, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.3682-14-2, Name is 6-Amino-2,3-dihydrophthalazine-1,4-dione, molecular formula is C8H7N3O2. In a article£¬once mentioned of 3682-14-2

[29] Enhanced chemiluminescent reactions catalyzed by horseradish peroxidase

Enhancement of light emission from the horseradish peroxidase-catalyzed oxidation of diacyl hydrazides on addition of 6-hydroxybenzothiazole or phenol derivatives forms the basis of rapid, specific, and sensitive chemiluminescent assays for peroxidase. The advantages and wide applicability of the technique have been demonstrated in a range of ligand-binding assays. Careful selection of chemiluminescent reagents, enhancer, their relative proportions and reaction conditions, and more detailed knowledge of the mechanism of enhancement should enable further improvements in sensitivity and the intensity or constancy of light emission.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N642 – PubChem