Tag: M.W:100-200

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 90-64-2, Name is 2-Hydroxy-2-phenylacetic acid, molecular formula is C8H8O3. In an article, author is Amano, Takayuki,once mentioned of 90-64-2, SDS of cas: 90-64-2.

Identification of enzymes responsible for dantrolene metabolism in the human liver: A clue to uncover the cause of liver injury

Dantrolene is used for malignant hyperthermia during anesthesia, and it sometimes causes severe liver injury as a side effect. Dantrolene is metabolized to acetylaminodantrolene, which is formed via the reduction of dantrolene to aminodantrolene and subsequent acetylation. Formation of hydroxylamine during the metabolic process may be associated with liver injury. We identified the enzymes responsible for dantrolene metabolism in humans to elucidate the mechanism of liver injury. Dantrolene reductase activity was not detected in human liver microsomes, but it was detected in cytosol. Formation was increased in the presence of N-1-methylnicotineamide, which is an electron donor to aldehyde oxidase 1 (AOX1). Potent inhibitors of AOX1 and a correlation study with a marker of AOX1 activity, namely phthalazine oxidase activity, in a panel of 28 human liver cytosol samples supported the role of AOX1 in dantrolene reduction. Acetylaminodantrolene formation from aminodantrolene was highly detected in recombinant N-acetyltransferase (NAT) 2 rather than NATI. A glutathione trapping assay revealed the formation of hydroxylamine via an AOX1-dependent reduction of dantrolene but not via hydroxylation of aminodantrolene. In conclusion, we found that AOX1 and NAT2 were responsible for dantrolene metabolism in humans and that AOX1-dependent metabolism determines dantrolene-induced liver injury.

Interested yet? Keep reading other articles of 90-64-2, you can contact me at any time and look forward to more communication. SDS of cas: 90-64-2.

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

Electric Literature of 62-23-7, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 62-23-7, Name is 4-Nitrobenzoic acid, SMILES is O=C(O)C1=CC=C([N+]([O-])=O)C=C1, belongs to phthalazine compound. In a article, author is Zhao, Xiao-Na, introduce new discover of the category.

A highly efficient and recyclable cobalt ferrite chitosan sulfonic acid magnetic nanoparticle for one-pot, four-component synthesis of 2H-indazolo[2,1-b]phthalazine-triones

A highly efficient magnetic CoFe2O4 chitosan sulfonic acid nanoparticle (CoFe2O4-CS-SO3H) was prepared and applied for one-pot, four-component synthesis of 2H-indazolo[2,1-b]phthalazine-triones by condensation of phthalic anhydride, hydrazinium hydroxide, 1,3-cyclohexanedione and aldehydes under solvent-free conditions at 80 degrees C. The magnetic nanocatalyst could be readily recovered by applying an external magnet and recycled several times without significant loss of its catalytic activity.

Electric Literature of 62-23-7, One of the oldest and most widely used commercial enzyme inhibitors is aspirin, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 62-23-7.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 140-75-0, Name is (4-Fluorophenyl)methanamine, formurla is C7H8FN. In a document, author is Coelho, Catarina, introducing its new discovery. Category: phthalazines.

Structural insights into xenobiotic and inhibitor binding to human aldehyde oxidase

Aldehyde oxidase (AOX) is a xanthine oxidase (XO)-related enzyme with emerging importance due to its role in the metabolism of drugs and xenobiotics. We report the first crystal structures of human AOX1, substrate free (2.6-angstrom resolution) and in complex with the substrate phthalazine and the inhibitor thioridazine (2.7-angstrom resolution). Analysis of the protein active site combined with steady-state kinetic studies highlight the unique features, including binding and substrate orientation at the active site, that characterize human AOX1 as an important drug-metabolizing enzyme. Structural analysis of the complex with the noncompetitive inhibitor thioridazine revealed a new, unexpected and fully occupied inhibitor-binding site that is structurally conserved among mammalian AOXs and XO. The new structural insights into the catalytic and inhibition mechanisms of human AOX that we now report will be of great value for the rational analysis of clinical drug interactions involving inhibition of AOX1 and for the prediction and design of AOX-stable putative drugs.

If you are hungry for even more, make sure to check my other article about 140-75-0, Category: phthalazines.

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

Reference of 620-14-4, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 620-14-4, Name is 3-Ethyltoluene, SMILES is CC1=CC(CC)=CC=C1, belongs to phthalazine compound. In a article, author is Gudala, Satish, introduce new discover of the category.

Facile synthesis of multi-functional 1,3,4-thiadiazine derivatives bearing phthalazine, pyridazine, and pyrido-pyridazine moieties

A series of novel, multifunctional 1,3,4-thiadiazine derivatives bearing phthalazines, pyridazines and pyrido-pyridazines (9-13) have been synthesized via the multicomponent reaction of (3-(2-bromo-2-[2-chloropyrimidin-4-yl]acetyl)-2-chlorophenyl)-2,6-dichloro benzene-sulfonamide with thiocarbohydrazide and various anhydrides. The reactions were performed by refluxing the components in mixed ethanol/acetic acid to afford the corresponding products in good to excellent yields. All the synthesized compounds were characterized by analytical and spectral studies. The developed method features short reaction time, simple work-up without chromatographic separation, and a broad range of substrate applicability.

Reference of 620-14-4, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 620-14-4 is helpful to your research.

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. 103-36-6, Name is Ethyl cinnamate, molecular formula is C11H12O2. In an article, author is Qin, Peiyong,once mentioned of 103-36-6, Recommanded Product: 103-36-6.

Preparation of a poly(phthalazine ether sulfone ketone) membrane with propanedioic acid as an additive and the prediction of its structure

In this study, propanedioic acid was investigated as a potential additive in poly(phthalazine ether sulfone ketone) (PPESK)/N-methyl-2-pyrrolidone solutions. Compared with poly(ethylene glycol) with a molecular weight of 1000 and Tween 80 as additives, different phenomena were observed: (1) both fingerlike and spongelike structures of asymmetric ultrafiltration membranes were induced by rapid gelation, and (2) a spongelike structure membrane with a high pure water flux was obtained under a high gelation rate. Moreover, the PPESK membrane formation process was recorded with a recently developed optical microscopy (OM)-charge-coupled device (CCD) camera experimental system. The predicted membrane structure with an OM-CCD system gave good correspondence with the final membrane structure and performance, as detected by scanning electron microscopy. (c) 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015, 132, 41621.

Interested yet? Keep reading other articles of 103-36-6, you can contact me at any time and look forward to more communication. Recommanded Product: 103-36-6.

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

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, Product Details of 24324-17-2, 24324-17-2, Name is 9-Fluorenemethanol, SMILES is C1=CC=CC3=C1C2=CC=CC=C2C3CO, belongs to phthalazine compound. In a document, author is Etinski, Mihajlo, introduce the new discover.

A theoretical study of low-lying singlet and triplet excited states of quinazoline, quinoxaline and phthalazine: insight into triplet formation

Quinazoline, quinoxaline and phthalazine are nitrogen containing heterocyclic aromatic molecules which belong to the class diazanaphthalenes. These isomers have low-lying n pi(star) and naphthalene-like pi pi(star) states that interact via spin-orbit coupling. In this contribution, we study their structure and electronic states by means of a coupled-cluster method. The computed properties are compared to those of cinnoline which were obtained in our previous study [Etinski et al., Phys. Chem. Chem. Phys., 2014, 16, 4740]. The excited state features of these isomers are dependent on the position of the nitrogen atoms. We find that quinazoline and quinoxaline exhibit similarities in the ordering and character of the excited states. In contrast, a marked difference in the electronic and geometric structures of the lowest excited triplet states of cinnoline and phthalazine is noticed, although both are orthodiazanaphthalenes. Our findings suggest that the S-1 (sic) T-1 channel is responsible for the rapid intersystem crossing in quinazoline and quinoxaline, whereas the S-1 (sic) T-2 pathway is active in phthalazine.

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 24324-17-2. Product Details of 24324-17-2.

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

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, 88-99-3, Name is Pathalic acid, SMILES is O=C(O)C1=CC=CC=C1C(O)=O, belongs to phthalazine compound. In a document, author is Abbasi, Armina, introduce the new discover, Name: Pathalic acid.

Time Course of Aldehyde Oxidase and Why It Is Nonlinear

Many promising drug candidates metabolized by aldehyde oxidase (AOX) fail during clinical trial owing to underestimation of their clearance. AOX is species-specific, which makes traditional allometric studies a poor choice for estimating human clearance. Other studies have suggested using half-life calculated by measuring substrate depletion to measure clearance. In this study, we proposed using numerical fitting to enzymatic pathways other than Michaelis-Menten (MM) to avoid missing the initial high turnover rate of product formation. Here, product formation over a 240-minute time course of six AOX substrates-O-6-benzylguanine, N-(2-dimethylamino)ethyl)acridine-4-carboxamide, zaleplon, phthalazine, BIBX1382 [N8-(3-Chloro-4-fluorophenyl)-N2-(1-methyl-4-piperidiny1)-pyrimido[5,4-d]pyrimidine-2,8-diamine dihydrochloride], and zoniporide-have been provided to illustrate enzyme deactivation over time to help better understand why MM kinetics sometimes leads to underestimation of rate constants. Based on the data provided in this article, the total velocity for substrates becomes slower than the initial velocity by 3.1-, 6.5-, 2.9-, 32.2-, 2.7-, and 0.2-fold, respectively, in human expressed purified enzyme, whereas the K-m remains constant. Also, our studies on the role of reactive oxygen species (ROS), such as superoxide and hydrogen peroxide, show that ROS did not significantly after the change in enzyme activity over time. Providing a new electron acceptor, 5-nitroquinoline, did, however, after the change in rate over time for mumerous compounds. The data also illustrate the difficulties in using substrate disappearance to estimate intrinsic clearance.

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 88-99-3 is helpful to your research. Name: Pathalic acid.

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

In an article, author is Simijonovic, Dusica, once mentioned the application of 371-42-6, Product Details of 371-42-6, Name is 4-Fluorothiophenol, molecular formula is C6H5FS, molecular weight is 128.17, MDL number is MFCD00004846, category is phthalazine. Now introduce a scientific discovery about this category.

A new efficient domino approach for the synthesis of pyrazolyl-phthalazine-diones. Antiradical activity of novel phenolic products

Pyrazolyl-phthalazine-dione derivatives (PPDs) were synthetized in the ionic liquid catalyzed one-pot multicomponent reaction of acetylacetone, 2,3-dihydrophthalazine-1,4-dione, and different aldehydes in moderate to good yields. Six new PPDs were obtained, and the crystal structure of 2-acetyl-1-(4-fluorophenyl)- 3-methyl-1H-pyrazolo[1,2-b] phthalazine-5,10-dione (PPD-4) was determined. The most interesting structural features of the novel PPD-4 is the formation of a rather short intermolecular distance between the F atom of one molecule and the midpoint of the neighbouring six-membered heterocyclic ring. This interaction arranges all molecules into parallel supramolecular chains. UV-Vis spectra of all PPDs were acquired and compared to the simulated ones obtained with TD-DFT. All synthetized compounds were subjected to evaluation of their in vitro antioxidative activity using a stable DPPH radical. It was shown that PPD-7, with a catechol motive, is the most active antioxidant, while PPD-9, with two neighbouring methoxy groups to the phenolic OH, exerted a somewhat lower, but significant antioxidative potential. The results of DFT thermodynamical study are in agreement with experimental findings that PPD-7 and PPD-9 should be considered as powerful radical scavengers. In addition, the obtained theoretical results (bond dissociation and proton abstraction energies) specify SPLET as a prevailing radical scavenging mechanism in polar solvents, and HAT in solvents with lower polarity. On the other hand, the obtained reaction enthalpies for inactivation of free radicals suggest competition between HAT and SPLET mechanisms, except in the case of the (OH)-O-center dot radical in polar solvents, where HAT is labeled as prefered.

If you are interested in 371-42-6, you can contact me at any time and look forward to more communication. Product Details of 371-42-6.

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

Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter.62-23-7, Name is 4-Nitrobenzoic acid, SMILES is O=C(O)C1=CC=C([N+]([O-])=O)C=C1, belongs to phthalazine compound. In a document, author is Boraei, Ahmed T. A., introduce the new discover, COA of Formula: C7H5NO4.

Design and synthesis of new phthalazine-based derivatives as potential EGFR inhibitors for the treatment of hepatocellular carcinoma

Searching for new leads in the battle of cancer will never ends, we herein disclose the design and synthesis of new phthalazine derivatives and their in vitro and in vivo testing for their antiproliferative activity. Phthalazine was selected as a privilege moiety that is incorporated in a big number of anticancer drugs in clinical use or that are still under clinical or preclinical studies. We utilized the drug extension strategy to tailor the designed compounds to fit the EGFR hydrophobic sub pocket and cleft region. The designed phthalazine derivatives was synthesized by linking phthalazine moiety with 1,3,4-oxadiazole-thione and 1,2,4-triazole-thione. Alkylation and glycosylation of the new heterocyclic systems were successfully performed to be used in the drug extension. Coupling of some phthalazine derivatives with different amino acids was also performed to improve the drug selectivity. The synthesized compounds were tested for their antiproliferative activity against cancer cells both in vivo and in vitro. The in vitro activity against hepatocellular carcinoma (HepG2 cell line) ranged from 5.7 mu g/mL to 43.4 mu g/mL. Compounds 31a and 16 were the most active with an IC(50)5.7 mu g/mL and 7.09 mu g/mL, respectively compared to the standard compound doxorubicin (4.0 mu g/mL). In vivo, compounds 10 and 16 showed IC50 values 7.25 mu g/mL and 7.5 mu g/mL, respectively compared to the standard compound cisplatin (IC50, 9.0 mu g/mL). In silico, testing of the phthalazine derivatives showed that they are good inhibitors for EGFR. The docking studies substantiated compounds 4, 10, 16 and 31a as new lead compounds and identified Arg841 as a key residue in the cleft region for binding stronger inhibitors.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 62-23-7. COA of Formula: C7H5NO4.

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

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , Formula: C9H7F3, 402-50-6, Name is 1-(Trifluoromethyl)-4-vinylbenzene, molecular formula is C9H7F3, belongs to phthalazine compound. In a document, author is Sanchez-Moreno, Manuel, introduce the new discover.

Phthalazine Derivatives Containing Imidazole Rings Behave as Fe-SOD Inhibitors and Show Remarkable Anti-T. cruzi Activity in Immunodeficient-Mouse Mode of Infection

A series of new phthalazine derivatives 1-4 containing imidazole rings were prepared. The monoalkylamino substituted. derivatives 2 and 4 were more active in vitro against T. cruzi and less toxic against Vero cells than both their disubstituted analogues and the reference drug benznidazole. Compounds 2 and 4 highly inhibited the antioxidant parasite enzyme Fe-SOD, and molecular modeling suggested that they interact with the H-bonding system of the iron atom moiety. In vivo tests on the acute phase of Chagas disease gave parasitemia inhibition values twice those of benznidazole, and a remarkable decrease in the reactivation of parasitemia was found in the chronic phase for immunodeficient mice. Glucose metabolism studies showed that compounds 1-4 did not affect the succinate pathway but originated important changes in the excretion of pyruvate metabolites. The morphological alterations found in epimastigotes treated with 1-4 confirmed extensive cytoplasm damage and a high mortality rate of parasites.

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 402-50-6. Formula: C9H7F3.

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