Category: 929-59-9

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, molecular formula is C6H16N2O2. In an article, author is Sawant-Basak, Aarti,once mentioned of 929-59-9, Product Details of 929-59-9.

Metabolism of a Serotonin-4 Receptor Partial Agonist 4-{4-[4-Tetrahydrofuran-3-yloxy)-Benzo[d]Isoxazol-3-yloxymethyl]-Piperidin-1-ylmethyl}-Tetrahydropyran-4-ol (TBPT): Identification of an Unusual Pharmacologically Active Cyclized Oxazolidine Metabolite in Human

4-{4-[4-Tetrahydrofuran-3-yloxy)-benzo[d]isoxazol-3-yloxymethyl]-piperidin-1-ylmethyl}-tetrahydropyran-4-ol (PF-4995274, TBPT) is a new agent that is a partial agonist of the human serotonin-4 (5-HT4) receptor and is under investigation for neurological disorders. Metabolism of TBPT was examined in vitro in human liver microsomes and human hepatocytes. Metabolites were also identified in the plasma of healthy human subjects in a phase 1 clinical study. Human-derived metabolite profiles were compared with corresponding profiles obtained in laboratory animal species. There were two major routes of metabolism in vitro: N-dealkylation of the methyltetrahydropyran moiety (M1) and hydroxylation at the seven position of the benzisoxazole moiety (M4). These were also observed in human plasma; however, in that matrix, the major metabolite was an unusual cyclized oxazolidine entity (M2). M2 was proposed to be formed via generation of an intermediate 4. iminium ion on the piperidine ring followed by spontaneous cyclization by attack of the beta-hydroxyl substituent of the tetrahydropyran ring to form a cyclized oxazolidine product. An authentic standard of the metabolite was generated using a methylene-blue-sensitized photochemical oxidation reaction as well as microbial transformation. Further investigation of this metabolite showed that it also possessed 5-HT4 agonism activity similar to the parent. The metabolite was 150-fold more highly protein bound in human plasma than TBPT, which is consistent with its presence as a major circulating metabolite while being only a minor metabolite in in vitro systems. Overall, this illustrates the importance of understanding the complex dispositional properties of a pharmacologically active metabolite. (C) 2013 Wiley Periodicals, Inc.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , Name: 1,2-Bis(2-aminoethoxy)ethane, 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, molecular formula is C6H16N2O2, belongs to benzisoxazole compound. In a document, author is Lee, SY, introduce the new discover.

Is subnanomolar binding affinity required for the in vivo imaging of acetylcholinesterase? Studies on F-18-labeled G379

Acetylcholinesterase (AChE) is an important cholinergic marker of Alzheimer’s disease (AD) and shows reduced activity in postmortem AD brain tissues. 1-(4-Fluorobenzyl)-4-[(5,6-dimethoxy-l-oxoindan-2-fluoro-2-yl)methyl]piperidine (G379, 1), an AChE inhibitor with a subnanomolar IC50 (0.56 nM), was prepared as a F-18-labeled radioligand ([F-18]1) and evaluated in mice. Metabolism studies of [F-18]1 showed no metabolites in the mouse brain. Tissue distribution studies demonstrated its uniform regional distribution in the mouse brain, suggesting that this radioligand is not suitable for the in vivo imaging of AChE. This result along with reports on radiolabeled AT-benzylpiperidine lactam benzisoxazole (IC50 < 1 nM) and other radiolabeled benzylpiperidme derivatives (IC50 > 1 nM) suggested that a subnanornolar IC50 may not be the only important factor in determining the suitability of a radioligand for in Vivo Studies of AChE. (c) 2006 Elsevier Inc. All rights reserved.

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 929-59-9. Name: 1,2-Bis(2-aminoethoxy)ethane.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

In an article, author is Marti, Sergio, once mentioned the application of 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, molecular formula is C6H16N2O2, molecular weight is 148.2034, MDL number is MFCD00040474, category is benzisoxazole. Now introduce a scientific discovery about this category, Quality Control of 1,2-Bis(2-aminoethoxy)ethane.

Are Heme-Dependent Enzymes Always Using a Redox Mechanism? A Theoretical Study of the Kemp Elimination Catalyzed by a Promiscuous Aldoxime Dehydratase

The design of biocatalysts is a goal to improve the rate, selectivity, and environmental friendliness of chemical processes in biotechnology. In this regard, the use of computational techniques has provided valuable assistance in the design of enzymes with remarkable catalytic activity. In this paper, hybrid QM/MM simulations have allowed getting an insight into the mechanism of a promiscuous aldoxime dehydratase (OxdA) for Kemp elimination. We first demonstrate that, based on the use of linear response approximation (LRA) methods, the lowest energy electronic state of the benzisoxazole placed in the active site of OxdA corresponds to a singlet state, the triplet and the quintet states being higher in energy. The presence of a heme group at the active site of the OxdA promiscuous enzyme opens the possibility of exploring a redox mechanism, similar to the one proposed in other reactions catalyzed by heme-dependent enzymes. In addition, according to the geometrical analysis of the active site of this aldoxime dehydratase, the presence of a good base in the active site, His320, the proper pose of the substrate assisted by the porphyrin, and an adequate electrostatic environment to stabilize the negative charge developed in the oxygen-leaving group makes available an acid/base mechanism. Comparison of the results derived from the exploration of both acid/base and redox mechanisms at the B3LYP(Def2-TZVP)/MM level shows how the latter renders the most favorable reaction path within the quintet state. The obtained activation free energy is in good agreement with the activation energy that can be deduced from the experimentally measured rate constant.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

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. 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, molecular formula is C6H16N2O2. In an article, author is Bruun, RD,once mentioned of 929-59-9, SDS of cas: 929-59-9.

Risperidone as a treatment for Tourette’s syndrome

Background: An open-label trial was performed to assess the efficacy and safety of risperidone, a benzisoxazole derivative with potent D-2 and 5-HT2 antagonism, for treatment of Tourette’s syndrome. Method: Thirty-eight patients with Tourette’s syndrome volunteered to take risperidone for treatment of their tics. All patients had failed to respond adequately to conventional treatments (with neuroleptics such as haloperidol and/or with the alpha(2)-adrenergic agonist clonidine) or had suffered from intolerable side effects from such treatments. Patients were rated for tic severity by the Yale Global Tic Severity Scale (YGTSS) before treatment and after 1 month of treatment with risperidone. Patients were monitored carefully for side effects and clinical response. Results: Of the 38 patients, 8 discontinued risperidone treatment before the end of the trial because of intolerable side effects. At the end of the 4-week trial, 22 patients (58%) were improved, 7 patients (18%) had no appreciable change in their symptoms, and 1 patient (3%) had a documented worsening of tics. Doses of risperidone at the end of the trial ranged from 0.5 mg to 9 mg/day (mean = 2.7 mg/day). Conclusion: This open clinical trial suggests that risperidone may be a promising alternative to conventional medications used for treating the symptoms of Tourette’s syndrome.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, Product Details of 929-59-9929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, SMILES is NCCOCCOCCN, belongs to Benzisoxazole compound. In a article, author is Iranpoor, Nasser, introduce new discover of the category.

A novel method for the highly efficient synthesis of 1,2-benzisoxazoles under neutral conditions using the Ph3P/DDQ system

The use of Ph3P/DDQ offers a novel, neutral and highly efficient method for the efficient conversion of 2-hydroxyaryl aldoximes and ketoximes to 1,2-benzisoxazoles in excellent yields at room temperature. (c) 2006 Published by Elsevier Ltd.

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 929-59-9. Product Details of 929-59-9.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Related Products of 929-59-9, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, SMILES is NCCOCCOCCN, belongs to Benzisoxazole compound. In a article, author is GenreGrandpierre, A, introduce new discover of the category.

Catalysis of the Kemp elimination by antibodies elicited against a cationic hapten

Rather efficient catalysis of the decomposition of 5-nitro-benzisoxazole to the cyanophenol was observed with antibodies elicited against a cationic hapten structurally unrelated to the benzisoxazole substrate. The rate enhancement by the most active antibody is better than 10(4) and the reaction is catalyzed by a carboxylate group associated with a hydrophobic binding site. (C) 1997 Elsevier Science Ltd.

Related Products of 929-59-9, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 929-59-9 is helpful to your research.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, molecular formula is , belongs to Benzisoxazole compound. In a document, author is Baglieri, Ausilia, Name: 1,2-Bis(2-aminoethoxy)ethane.

Competitive Copper Catalysis in the Condensation of Primary Nitro Compounds with Terminal Alkynes: Synthesis of Isoxazoles

Isoxazoles, mainly 3,5-disubstituted, are prepared by catalytic condensation of primary nitro compounds with terminal acetylenes by using a copper/base catalytic system. The additional catalytic effect of the copper(II) salts is evidenced by comparing the kinetic profiles. Selectivity dependence on reaction conditions is considered for phenylacetylene in the following competitive processes: oxidative coupling of terminal alkynes to conjugated diynes catalyzed by Cu-II and base in the presence of air; production of furazans beside condensation with benzoylnitromethane to 3-benzoylisoxazoles, as a result of the reaction of the dipolarophile with 3,4-dibenzoylfuroxan; addition of electron-poor alkynes (e.g., methyl propiolate) with themselves and with the nitro compound. Thus, oxidative coupling is negligible in reactions with active nitro compounds, whereas with nitroalkanes both products are observed: only trace amounts of isoxazoles are detected without copper. Similarly, in the presence of copper, 3-benzoyl-5-phenylisoxazole is predominant over the furazan. Furthermore, condensations of electron-poor alkynes give complex reaction mixtures in the presence of base alone, but cycloadducts are conveniently prepared with copper. The results indicate the practical and general utility of this catalytic method for synthetic practice.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 929-59-9, in my other articles. Name: 1,2-Bis(2-aminoethoxy)ethane.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Chen, Ying, once mentioned the application of 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, molecular formula is C6H16N2O2, molecular weight is 148.2034, MDL number is MFCD00040474, category is Benzisoxazole. Now introduce a scientific discovery about this category, SDS of cas: 929-59-9.

Genotyping as a Key Element of Sample Size Optimization in Bioequivalence of Risperidone Tablets

Risperidone is a derivative of benzisoxazole and is widely used for schizophrenia and other psychiatric illnesses in both adults and children. Previous studies have confirmed that it is a highly variable drug (within-subject variability >= 30%). To reduce the large sample size required for bioequivalence researches on highly variable drugs, a role for genotyping in the design of the bioequivalence study was employed. A randomized, open-label, two-period crossover study was adopted: 20 subjects with specific genotypes carrying cytochrome P450 (CYP) 2D6*10 were randomized to two groups to receive a single oral dose of trial formulation or reference formulation with a 2-week washout period. Blood concentrations of risperidone (parent drug) and 9-hydroxy risperidone (active metabolite) were measured by high-performance liquid chromatography-tandem mass spectrometry. Eighteen out of the 20 subjects completed the study (two did not finish the test in the second period). The pharmacokinetic parameters of AUC(last), AUC(a) and C (max) for the 18 subjects after a single oral dose of the trial or reference preparation were 216.1 +/- 88.7 and 220.5 +/- 96.8 ng center dot h/mL; 221.6 +/- 93.1 and 226.4 +/- 103.5 ng center dot h/mL; 36.7 +/- 10.3 and 36.0 +/- 10.2 ng/mL, respectively. The CVw of risperidone in natural logarithm-transformed C (max) was 22.4 and 25.38% for 9-hydroxy risperidone. The test formulation met the Food and Drug Administration guidelines and regulation criteria for bioequivalence. By controlling the genotype, it could actually help reduce the CVw, which may be a feasible method to decrease the sample size for the bioequivalence study of highly variable drugs.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

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. 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, formurla is C6H16N2O2. In a document, author is Bhaskarachar, Ravi Kiran, introducing its new discovery. HPLC of Formula: C6H16N2O2.

Design, synthesis and anticancer activity of functionalized spiro-quinolines with barbituric and thiobarbituric acids

A new series of spiro-quinoline compounds have been accomplished by the reaction of barbituric acid or thiobarbituric acid with derivatives of benzisoxazole-5-carbaldehyde or 2-substituted benzaldehyde. These compounds were evaluated for their in vitro cytotoxicity on two mammalian cancer cell lines MCF-7 and KB. The compounds exhibit cytotoxicity against these cell lines in micromolar range. Among the series of compounds, 11(a-j) particularly 11b and 11e showed relatively good activity against both the tested cell lines. Compound 11b was found to exhibit the highest cytotoxic activity with IC50 value 90.2 mu M for MCF-7 and 49.8 mu M for KB cell line. Flow cytometric analysis study confirmed that these molecules induced cytotoxicity via apoptosis.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry, like all the natural sciences, Category: Benzisoxazole, begins with the direct observation of nature¡ª in this case, of matter.929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, SMILES is NCCOCCOCCN, belongs to Benzisoxazole compound. In a document, author is Li, Jing, introduce the new discover.

Determination of zonisamide by a coated monolithic column

In this paper, a monolithic ODS-silica gel column dynamically coated with cetylpyridinium chloride (CPC) was used to demonstrate the high-speed and efficient separation of zonisamide (1,2-benzisoxazole-3-methanesulfonamide, ZNS). its raw material (1,2-benzisoxazole-3-methanecarbonic acid) and intermediate (sodium 1,2-benzisoxazole-3-methanesulfonate) in drugs. Using a 40 mmol/L sodium perchlorate solution (pH 7.0) containing 10% acetonitrile as eluent, the analytes were eluted with a sharp and symmetrical peak within 3.0 min, detected with UV detection at 210 nm. The column demonstrates excellent stability over time, and exhibits unusual selectivity for pharmaceutical analysis. Thus, by this developed method, zonisamide in drug samples can be determined rapidly with high recoveries and good selectivity. (c) 2006 Elsevier B.V. All rights reserved.

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 929-59-9. Category: Benzisoxazole.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics