Category: 14348-75-5

Chemistry, like all the natural sciences, begins with the direct observation of nature¡ª in this case, of matter.14348-75-5, Name is 2,7-Dibromo-9H-fluoren-9-one, SMILES is C3=C2C1=C(C=C(Br)C=C1)C(C2=CC(=C3)Br)=O, belongs to phthalazines compound. In a document, author is Qin Xingyu, introduce the new discover, Quality Control of 2,7-Dibromo-9H-fluoren-9-one.

Synthesis of hydralazine-N-lactose and its metabolites in vitro

Hydralazine-N-lactose is a main impurity in hydralazine tablets. Hydralazine and lactose were used as raw materials, and silica gel column and preparation column of octadecylsilane bonded silica were selected to prepare and purify hydralazine-N-lactose. Its in vitro metabolites were identified by utilizing SD rat liver microsomes. The results of samples in vitro were compared with blank group and the resulting metabolites structures were identified by LC-MS/MS. Hydrazine-N-lactose produced six main metabolites, including s-triazolo[3, 4-a] phthalazine, 3 -methyl-s-triazolo [3, 4-a] phthalazine, 3 -(1-hydroxy) methyl-s-triazolo [3, 4-a] phthalazine, 3 hydroxymethyl-s-triazolo[ 3, 4-a] phthalazine, hydralazine and dehydro-hydralazine-N-lactose after in vitro metabolism. This study will be valuable in hydralazine-lactose conjunctions metabolism research and hydralazine formulation safety.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 14348-75-5 is helpful to your research. Quality Control of 2,7-Dibromo-9H-fluoren-9-one.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Reference of 14348-75-5, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 14348-75-5, Name is 2,7-Dibromo-9H-fluoren-9-one, SMILES is C3=C2C1=C(C=C(Br)C=C1)C(C2=CC(=C3)Br)=O, belongs to phthalazines compound. In a article, author is Romero, Angel H., introduce new discover of the category.

Anticancer potential of new 3-nitroaryl-6-(N-methyl)piperazin-1,2,4-triazolo[3,4-a]phthalazines targeting voltage-gated K+ channel: Copper-catalyzed one-pot synthesis from 4-chloro-1-phthalazinyl-arylhydrazones

A series of six 3-aryl-6-(N-methylpiperazin)-1,2,4-triazolo[3,4-a]phthalazines were prepared through a facile and efficient one-pot copper-catalyzed procedure from 4-chloro-1-phthalazinyl-arylhydrazones with relatively good yields (62-83%). The one-pot copper-catalytic procedure consists of two simultaneous reactions: (i) a direct intramolecular dehydrogentaive cyclization between ylidenic carbon and adjacent pyrazine nitrogen to form 1,2,4-triazolo ring and, (ii) a direct N-amination on carbon-chlorine bond. Then, an in vitro anticancer evaluation was performed for the synthesized compounds against five selected human cancer cells (A549, MCF-7, SKBr3, PC-3 and HeLa). The nitro-derivatives were significantly more active against cancer strains than against the rest of tested compounds. Specifically, compound 8d was identified as the most promising anticancer agent with significant biological responses and low relative toxicities on human dermis fibroblast. The cytotoxic effect of compound 8d was more significant on PC3, MCF-7 and SKBr3 cancer cells with low-micromolar IC50 value ranging from 0.11 to 0.59 mu M, superior to Adriamycin drug. Mechanistic experimental and theoretical studies demonstrated that compounds 8d act as a K+ channel inhibitor in cancer models. Further molecular docking studies suggest that the EGFR Tyrosine Kinase enzyme may be a potential target for the most active 3-aryl-6-(N-methylpiperazin)-1,2,4-triazolo[3,4-a]phthalazines.

Reference of 14348-75-5, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 14348-75-5.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

In an article, author is Han, Lyrialle W., once mentioned the application of 14348-75-5, Recommanded Product: 2,7-Dibromo-9H-fluoren-9-one, Name is 2,7-Dibromo-9H-fluoren-9-one, molecular formula is C13H6Br2O, molecular weight is 337.99, MDL number is MFCD00010790, category is phthalazines. Now introduce a scientific discovery about this category.

Effect of N-Acetyltransferase 2 Genotype on the Pharmacokinetics of Hydralazine During Pregnancy

Hydralazine, an antihypertensive agent used during pregnancy, undergoes N-acetylation primarily via N-acetyltransferase 2 (NAT2) to form 3-methyl-1,2,4-triazolo[3,4-a]phthalazine (MTP). To characterize the steady-state pharmacokinetics (PK) of hydralazine during pregnancy and evaluate the effects of NAT2 genotype on hydralazine and MTP PK during pregnancy, 12 pregnant subjects received oral hydralazine (5-25 mg every 6 hours) in mid- (n = 5) and/or late pregnancy (n = 8). Serial blood samples were collected over 1 dosing interval, and steady-state noncompartmental PK parameters were estimated. Subjects were classified as either (rapid acetylators, n = 6) or slow acetylators (SAs, n = 6) based on NAT2 genotype. During pregnancy, when compared with the SA group, the RA group had faster weight-adjusted hydralazine apparent oral clearance (70.0 +/- 13.6 vs 20.1 +/- 6.9 L/h, P .05), lower dose-normalized area under the concentration-time curve (AUC; 1.5 +/- 0.8 vs 5.9 +/- 3.7 ng center dot h/mL, P .05), lower dose-normalized peak concentrations (0.77 +/- 0.51 vs 4.04 +/- 3.18 ng/mL, P .05), and larger weight-adjusted apparent oral volume of distribution (302 +/- 112 vs 116 +/- 45 L/kg, P .05). Furthermore, the MTP/hydralazine AUC ratio was similar to 10-fold higher in the RA group (78 +/- 30 vs 8 +/- 3, P .05) than in the SA group. No gestational age or dose-dependent effects were observed, possibly because of the small sample size. This study describes for the first time, the PK of oral hydralazine and its metabolite, MTP, during pregnancy, and confirmed that the PK of oral hydralazine is NAT2 genotype dependent during pregnancy.

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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Reference of 14348-75-5, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 14348-75-5, Name is 2,7-Dibromo-9H-fluoren-9-one, SMILES is C3=C2C1=C(C=C(Br)C=C1)C(C2=CC(=C3)Br)=O, belongs to phthalazines compound. In a article, author is Mohamadpour, Farzaneh, introduce new discover of the category.

Four-component clean process for the eco-friendly synthesis of 1H-pyrazolo [1,2-b]phthalazine-5,10-dione derivatives using Zn(OAc)(2)center dot 2H(2)O as an efficient catalyst under solvent-free conditions

An efficient and convenient zinc acetate dihydrate (Zn(OAc)(2)center dot 2H(2)O) catalyzed synthesis of 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivatives has been accomplished via one-pot four-condensation of phthalic anhydride, hydrazine monohydrate, aromatic aldehydes derivatives and malononitrile under solvent-free conditions. The notable advantages of the present procedure are: operational simplicity, eco-friendly, environmentally benign nature, low-cost and non-toxic catalyst, no necessity of chromatographic purification steps, short reaction times and good to high yields.

Reference of 14348-75-5, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 14348-75-5.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 14348-75-5, Name is 2,7-Dibromo-9H-fluoren-9-one, molecular formula is C13H6Br2O. In an article, author is Sangshetti, Jaiprakash,once mentioned of 14348-75-5, Safety of 2,7-Dibromo-9H-fluoren-9-one.

Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review

Phthalazine, a structurally and pharmacologically versatile nitrogen-containing heterocycle, has gained more attention from medicinal chemists in the design and synthesis of novel drugs owing to its pharmacological potential. In particular, phthalazine scaffold appeared as a pharmacophoric feature numerous drugs exhibiting pharmacological activities, in particular, antidiabetic, anticancer, antihypertensive, antithrombotic, anti-inflammatory, analgesic, antidepressant and antimicrobial activities. This review presents a summary of updated and detailed information on phthalazine as illustrated in both patented and non-patented literature. The reported literature have described the optimal pharmacological characteristics of phthalazine derivatives and highlighted the applicability of phthalazine, as potent scaffold in drug discovery.

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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 14348-75-5, Name is 2,7-Dibromo-9H-fluoren-9-one, SMILES is C3=C2C1=C(C=C(Br)C=C1)C(C2=CC(=C3)Br)=O, belongs to phthalazines compound. In a document, author is Bourne, Christina R., introduce the new discover, Product Details of 14348-75-5.

Structure-activity relationship for enantiomers of potent inhibitors of B. anthracis dihydrofolate reductase

Background: Bacterial resistance to antibiotic therapies is increasing and new treatment options are badly needed. There is an overlap between these resistant bacteria and organisms classified as likely bioterror weapons. For example, Bacillus anthracis is innately resistant to the anti-folate trimethoprim due to sequence changes found in the dihydrofolate reductase enzyme. Development of new inhibitors provides an opportunity to enhance the current arsenal of anti-folate antibiotics while also expanding the coverage of the anti-folate class. Methods: We have characterized inhibitors of B. anthracis dihydrofolate reductase by measuring the K-i and MIC values and calculating the energetics of binding. This series contains a core diaminopyrimidine ring, a central dimethoxybenzyl ring, and a dihydrophthalazine moiety. We have altered the chemical groups extended from a chiral center on the dihydropyridazine ring of the phthalazine moiety. The interactions for the most potent compounds were visualized by X-ray structure determination. Results: We find that the potency of individual enantiomers is divergent with clear preference for the S-enantiomer, while maintaining a high conservation of contacts within the binding site. The preference for enantiomers seems to be predicated largely by differential interactions with protein residues Leu29, Gln30 and Arg53. Conclusions: These studies have clarified the activity of modifications and of individual enantiomers, and highlighted the role of the less-active R-enantiomer in effectively diluting the more active S-enantiomer in racemic solutions. This directly contributes to the development of new antimicrobials, combating trimethoprim resistance, and treatment options for potential bioterrorism agents. Published by Elsevier B.V.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 14348-75-5 is helpful to your research. Product Details of 14348-75-5.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Electric Literature of 14348-75-5, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 14348-75-5, Name is 2,7-Dibromo-9H-fluoren-9-one, SMILES is C3=C2C1=C(C=C(Br)C=C1)C(C2=CC(=C3)Br)=O, belongs to phthalazines compound. In a article, author is Turhan, K., introduce new discover of the category.

Efficient One-Pot Synthesis of 2H-indazolo[2,1-b]phthalazine-1,6,11-trione Derivatives Catalyzed by Y(OTf)(3)

In this study, substituted 2H-indazolo[2,1-b]phthalazine-1,6,11-triones, that may possess biological activity, have been synthesized via one-pot three-component cyclocondensation reaction of aromatic aldehydes, cyclic 1,3-dione and phthalhydrazide in ethanol catalyzed by Y(OTf)(3) with good to excellent yields. The structures of all synthesized compounds, 3,4-dihydro-13-phenyl-2H-indazolo[2,1-b]phthalazine-1,6,11(13H)-trione (4a), 13-(4-cyanophenyl)-3,4-dihydro-2H-indazolo[2,1-b]phthalazine-1,6,11(13H)-trione (4b), 3,4-dihydro-3,3-dimethyl-13-(4-cyanophenyl)-2H-indazolo[2,1-b]phthalazine-1,6,11(13H)-trione (4c), 3,4-dihydro-3,3-dimethyl-13-phenyl-2H-indazolo[2,1-b]phthalazine-1,6,11(13H)-trione (4d), and 3,4-dihydro-13-(4-isopropylphenyl)-3,3-dimethyl-2H-indazolo[2,1-b]phthalazine-1,6,11(13H)-trione (4e) have been elucidated from IR, NMR and mass spectral data.

Electric Literature of 14348-75-5, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 14348-75-5 is helpful to your research.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem

Chemistry is an experimental science, Computed Properties of C13H6Br2O, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 14348-75-5, Name is 2,7-Dibromo-9H-fluoren-9-one, molecular formula is C13H6Br2O, belongs to phthalazines compound. In a document, author is Rizk, Sameh A..

Design, Regiospecific Green Synthesis, Chemical Computational Analysis, and Antimicrobial Evaluation of Novel Phthalazine Heterocycles

Phthalazines have received considerable attention for their wide antimicrobial activity. Regiospecific nucleophilic attack of 4-benzylphthalazin-1-ol by the 1-oxo rather than the aza group on different alkyl halides gave novel phthalazine heterocyclic derivatives. Moreover, a variety of nucleosides bonded to electron-withdrawing groups were synthesized using 4-benzylphthalazine-1-ol. The density functional theory has been used to investigate the electronic structure of the synthesized compounds. All of the synthesized derivatives showed remarkable activity when tested against Gram-positive and Gram-negative bacteria, Aspergillus niger, and Candida albicans. The reactivity of these nucleosides was expected to arise from their bonding with the lone pair of N-atom of the macromolecules of bacteria. These bonding were expected to inhibit the enzyme by forming highly stable complex with lower highest occupied molecular orbital energy. The structures of these synthesized derivatives were established by Fourier transform infrared, H-1-NMR, and C-13-NMR spectroscopic evidence.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 14348-75-5. Computed Properties of C13H6Br2O.

Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem