Month: March 2021

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. 113-24-6, Name is Sodium pyruvate, molecular formula is , belongs to Benzisoxazole compound. In a document, author is STIFF, DD, Name: Sodium pyruvate.

REDUCTIVE METABOLISM OF THE ANTICONVULSANT AGENT ZONISAMIDE, A 1,2-BENZISOXAZOLE DERIVATIVE

1. The metabolism of zonisamide in vitro was characterized through aerobic and anaerobic incubations with rat liver subcellular fractions and cultured gastrointestinal microflora. 2. Zonisamide reacted with rat hepatic microsomal cytochrome P-450 and exhibited a Type I binding spectrum. 3. Metabolism of zonisamide in vitro by hepatic subcellular fractions and cultured gastrointestinal flora produced a single metabolite, 2-(sulphamoylacetyl)-phenol (2-SMAP), by reductive cleavage of the 1,2-benzisoxazole ring. 4. The reductive metabolism of zonisamide was primarily mediated by microsomal cytochrome P-450. The soluble fraction enhanced reduction when combined with the microsomal fraction but itself possessed only weak reductive activity. 5. Reduction of zonisamide by the most enzymically active liver fractions required NADPH, was stimulated by FMN and SKF-525A, and was inhibited by CO or air, as well as by n-octylamine. 6. Unlike their involvement in the reduction of numerous nitro, azo, and N-oxide compounds, cultured aerobic and anaerobic intestinal flora were not principally involved in the reduction of zonisamide.

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 113-24-6, in my other articles. Name: Sodium pyruvate.

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

In an article, author is MEWSHAW, RE, once mentioned the application of 3878-55-5, COA of Formula: C5H8O4, Name is 4-Methoxy-4-oxobutanoic acid, molecular formula is C5H8O4, molecular weight is 132.12, MDL number is MFCD00002788, category is Benzisoxazole. Now introduce a scientific discovery about this category.

EXAMINATION OF THE D(2)/5-HT(2) AFFINITY RATIOS OF RESOLVED 5,6,7,8,9,10-HEXAHYDRO-7,10-IMINOCYCLOHEPT[B]INDOLES – AN ENANTIOSELECTIVE APPROACH TOWARD THE DESIGN OF POTENTIAL ATYPICAL ANTIPSYCHOTICS

Enantiomers of several N-substituted 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles were obtained by the resolution of 2-fluoro-5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indole and 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indole followed by N-alkylation. These, as well as the racemates, were evaluated for their affinity for the 5-HT2 and D2 receptors. Those compounds possessing the 7S,10R stereochemistry were consistently recognized by the 5-HT2 and D2 receptors as the eutomer. 2-Fluoro-11-[4-(4-fluorophenyl)-4-oxobutyl]-5,6,7,8,9,10-hexahydro-7S,10R-iminocyclohept[b]indole [(7S,10R)-8] had the highest affinity for the 5-HT2 receptor (K(i) = 0.80 nM), while its distomer (7R,10S)-8 was the most selective member of this class of bridged gamma-carbolines (D2/5-HT2 = 562). Incorporation of a benzoyl or isosteric benzisoxazole moiety tethered by a four-carbon spacer to a bridged gamma-carboline nucleus, possessing the 7S,10R absolute configuration, produced high affinity ligands for the 5-HT2 and D2 receptors.

If you are interested in 3878-55-5, you can contact me at any time and look forward to more communication. COA of Formula: C5H8O4.

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 Bhana, N, once mentioned the application of 719-64-2, Name is 5-Chloro-3-phenylbenzo[c]isoxazole, molecular formula is C13H8ClNO, molecular weight is 229.66, MDL number is MFCD00014573, category is Benzisoxazole. Now introduce a scientific discovery about this category, Recommanded Product: 5-Chloro-3-phenylbenzo[c]isoxazole.

Risperidone – A review of its use in the management of the behavioural and psychological symptoms of dementia

Risperidone is a benzisoxazole derivative which has proven efficacy against the positive and negative symptoms of schizophrenia It has mon recently been investigated and shown efficacy as a treatment for the behavioural and psychological symptoms associated with dementia in the elderly. Risperidone has pharmacological properties resembling those of the atypical antipsychotic clozapine and an improved tolerability profile compared with the conventional antipsychotic haloperidol. Risperidone has antagonistic activity primarily at serotonin 5-HT2A and dopamine D-2 receptors. In the first 2 large, well controlled trials of an antipsychotic agent used in the treatment of elderly patients with Alzheimer’s dementia, vascular dementia or mixed demential risperidone 1 mg/day was at least as effective as haloperidol and superior to placebo. as assessed by the rating scales for global behaviour, aggression and psychosis. In extension phases of the 2 trials, clinical benefits were maintained for treatment periods of up to 1 year, with an incidence rate of tardive dyskinesia (2.6%) one-tenth of that seen with conventional antipsychotics. Risperidone, administered at a low dosage of 1 mg/day was associated with fewer extrapyramidal symptoms compared with haloperidol in elderly patients, Risperidone was well tolerated with no clinically relevant abnormalities in laboratory tests. vital signs or electrocardiogram results. Conclusion: The efficacy of risperidone has been demonstrated in the treatment of the behavioural and psychological symptoms associated with dementia in the elderly. Preliminary results from 1-year extension studies confirm the favourable efficacy and tolerability profile of risperidone 1 mg/day, Although head to head studies with other atypical antipsychotic agents are required and the long term use of the drug requires clarification, risperidone represents a generally well tolerated and effective treatment in the management of dementia-associated behavioural and psychological symptoms in the elderly.

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

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 868-14-4, Name is Potassium hydrogen tartrate, molecular formula is C4H5KO6, belongs to Benzisoxazole compound, is a common compound. In a patnet, author is Crabtree, Brian L., once mentioned the new application about 868-14-4, Recommanded Product: 868-14-4.

Iloperidone for the Management of Adults with Schizophrenia

Background: Iloperidone is a second-generation antipsychotic drug approved in May 2009 by the US Food and Drug Administration (FDA) for the acute treatment of schizophrenia in adults. It is a piperidinyl-benzisoxazole derivative with mixed serotonin (5HT2A) and D2 dopamine antagonist properties. Objective: The purpose of this article was to review the pharmacology, pharmacokinetics, efficacy, safety, and role in treatment for iloperidone in schizophrenia. Methods: Scientific and clinical data were collected through searches of PubMed, ClinicalTrials.gov, International Pharmaceutical Abstracts, and the FDA, using the search term iloperidone, and limited to English-language articles. Reference lists were reviewed for additional publications. Dates included the beginning of the database through 2010. No limits were placed on study design. Results: In a 4-week Phase III trial, iloperidone 12 mg twice daily lowered the Positive and Negative Syndrome Scale (PANSS) total scores to a significantly greater extent than did placebo (-12 vs -7.1; P < 0.01). The ziprasidone active control also separated from placebo (-12.3 vs -7.1; P < 0.05). A pooled analysis of 3 Phase III trials compared iloperidone in divided doses to placebo. The primary outcome was reduction in PANSS scores. Study 1 included iloperidone 4, 8, or 12 mg/d, haloperidol as an active control, and placebo. The PANSS reduction in the 12 mg/d group was significantly greater at end point versus baseline when compared with placebo (-9.9 vs -4.6; P = 0.047). Study 2 included iloperidone 4 to 8 mg/d or 10 to 16 mg/d, risperidone 4 to 8 mg/d, or placebo. The primary efficacy measure was change from baseline to end point in the Brief Psychiatric Rating Scale (BPRS). Improvement from baseline on all iloperidone doses was significantly greater than with placebo (4-8 mg/d group: -6.2, P = 0.012; 10-16 mg/d group: -7.2, P = 0.001; placebo, -2.5). Study 3 included iloperidone 12 to 16 mg/d, risperidone 6 to 8 mg/d, and placebo. The results on the primary efficacy variable, reduction in the BPRS score, was not significant for the 12 to 16 mg/d group versus placebo (-7.1 vs -5.0; P = 0.09), but was significant for the 20 to 24 mg/d iloperidone group (-8.6 vs -5.0; P = 0.01) and for the risperidone group (-11.5 vs 5.0; P < 0.001). A 52-week maintenance trial included iloperidone versus haloperidol as an active control. The primary efficacy variable was time to relapse. Comparison of mean time to relapse of the 2 arms showed no significant difference. The most common adverse events (AEs) associated with iloperidone were dizziness (5.1%-23.2%), dry mouth (5.2%-10.4%), somnolence (4%-13%), and dyspepsia (4.8%-7.8%). AEs appeared dose related. Prescribing information recommends a starting dosage of 1 mg twice daily and then titrated over 7 days to reach a target dosage of 12 to 24 mg/d. The titration is necessary to reduce the risk of orthostatic hypotension-related dizziness. Conclusions: Data support that when titrated slowly to a therapeutic dosage, iloperidone is generally well tolerated, has a favorable safety profile, and is an effective treatment option in patients with schizophrenia. Its place in therapy and performance in a typical patient population remain to be established. Slow initial titration and twice-daily dosing are potential disadvantages. (Clin Ther. 2011;33:330-345) (C) 2011 Published by Elsevier HS Journals, Inc. We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 868-14-4. The above is the message from the blog manager. Recommanded Product: 868-14-4.

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

In an article, author is Safaei-Ghomi, Javad, once mentioned the application of 15026-17-2, COA of Formula: C8H14O4, Name is 4-(tert-Butoxy)-4-oxobutanoic acid, molecular formula is C8H14O4, molecular weight is 174.19, MDL number is MFCD00273441, category is Benzisoxazole. Now introduce a scientific discovery about this category.

A convenient method for the preparation of 2-aminobenzophenone derivatives under ultrasonic irradiation

A quick and convenient method for the preparation of 2-aminobenzophenone derivatives is described. This approach consists of the nucleophilic substitution reaction of nitrobenzenes by phenylacetonitrile under conventional and ultrasonic conditions followed by reduction of the produced 2,1-benzisoxazole to 2-aminobenzophenone. This 2-step reaction was studied by changing the reaction parameters (reaction temperature, ultrasound power, and reaction time). The results clearly demonstrated that using ultrasound irradiation results in a high yield within a short reaction time.

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

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 133-37-9, Name is (2R,3R)-rel-2,3-Dihydroxysuccinic acid. In a document, author is Zheng, L, introducing its new discovery. Recommanded Product: (2R,3R)-rel-2,3-Dihydroxysuccinic acid.

Mechanistic study of proton transfer and hysteresis in catalytic antibody 16E7 by site-directed mutagenesis and homology modeling

Antibody 16E7 catalyzes the carbon protonation of enol ether 2 to hemiacetal 3, and the carbon deprotonation of benzisoxazole 7 to phenol 8. This antibody shows an extreme case of hysteresis, requiring several hours to reach full activity. Antibody 16E7 was expressed as recombinant chimeric Fab in Escherichia coli. A model for the three-dimensional structure was produced by homology modeling and used for a docking procedure to obtain models for antibody-ligand complexes. Site-direct mutagenesis of Glu(L39), identified as a possible catalytic residue by the model, to either glutamine or alanine abolished catalysis, showing that both the protonation reaction of enol ether 2 and the deprotonation of benzisoxazole 7 are promoted by the same residue. The model furthermore suggested that substrate access to the catalytic site might be hindered by a flexible HCDR3 loop held in closed position by a hydrogen bond between Ser(H99) and Glu(L39), which could explain the observed hysteresis effect. In agreement with this model, mutagenesis of Ser(H99) to alanine, or deletion of this residue, was found to reduce hysteresis by approximately 50%. (C) 2004 Elsevier Ltd. All rights reserved.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 133-37-9 help many people in the next few years. Recommanded Product: (2R,3R)-rel-2,3-Dihydroxysuccinic acid.

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

Application of 181289-15-6, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 181289-15-6, Name is 3-(2-Amino-2-oxoethyl)-5-methylhexanoic acid, SMILES is CC(C)CC(CC(N)=O)CC(O)=O, belongs to Benzisoxazole compound. In a article, author is Acosta-Silva, Carles, introduce new discover of the category.

Kemp Elimination Reaction Catalyzed by Electric Fields

The Kemp elimination reaction is the most widely used in the de novo design of new enzymes. The effect of two different kinds of electric fields in the reactions of acetate as a base with benzisoxazole and 5-nitrobenzisoxazole as substrates have been theoretically studied. The effect of the solvent reaction field has been calculated using the SMD continuum model for several solvents; we have shown that solvents inhibit both reactions, the decrease of the reaction rate being larger as far as the dielectric constant is increased. The diminution of the reaction rate is especially remarkable between aprotic organic solvents and protic solvents as water, the electrostatic term of the hydrogen bonds being the main factor for the large inhibitory effect of water. The presence of an external electric field oriented in the direction of the charge transfer (z axis) increases it and, so, the reaction rate. In the reaction of the nitro compound, if the electric field is oriented in an orthogonal direction (x axis) the charge transfer to the NO2 group is favored and there is a subsequent increase of the reaction rate. However, this increase is smaller than the one produced by the field in the z axis. It is worthwhile mentioning that one of the main effects of external electric fields of intermediate intensity is the reorientation of the reactants. Finally, the implications of our results in the de novo design of enzymes are discussed.

Application of 181289-15-6, 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 181289-15-6 is helpful to your research.

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

Reference of 127-17-3, 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. 127-17-3, Name is 2-Oxopropanoic acid, SMILES is CC(C(O)=O)=O, belongs to Benzisoxazole compound. In a article, author is Liu, KH, introduce new discover of the category.

High-performance liquid chromatographic assay of zonisamide (1,2-benzisoxazole-3-methanesulfonamide) in human plasma using a solid-phase extraction technique

A selective and sensitive liquid chromatographic method was developed for the determination of zonisamide in small volumes of plasma. Zonisamide and the internal standard methyl 4-hydroxybenzoate were extracted from 0.2 mL. of plasma with solid-phase extraction columns and eluted with methanol. Analysis of the extracts was performed on a Symmetry C-18 column with ultra-violet spectrophotometric detection. The calibration curve was linear over the concentration range of 0.05-5 mug mL(-1) in plasma. Recoveries were reasonable for routine analyses; the limit of quantification was 0.05 mug mL(-1) with a signal-to-noise ratio of 5. This method could be useful for the pharmacokinetic study of zonisamide in a limited volume of human plasma and for therapeutic drug monitoring.

Reference of 127-17-3, 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 127-17-3 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. 6009-70-7, Name is Ammonium oxalate monohydrate, molecular formula is , belongs to Benzisoxazole compound. In a document, author is FERRIS, DC, Recommanded Product: 6009-70-7.

RATE OF DECARBOXYLATION OF BENZISOXAZOLE-3-CARBOXYLATE IONS AS A PROBE OF SOLVATION IN BIOLOGICAL AND OTHER MEDIA

The influence of solvent donor-acceptor properties and polarity on the rates of decarboxylation of benzisoxazole-3-carboxylate ions is analyzed with the unified solvation model. When the dissolved species is a separated ion pair, solvent polarity decreases the rate. When an equilibrium exists between an ion pair and the dissociated ion pair, solvent polarity and donor strength increase the rate by increasing the extent of dissociation. Hydrogen bonding to the carboxylate functionality causes a significant decrease in rate. When using this probe to measure the solvation properties of solvents, micelles, polymers, or biological assemblies, these different effects must be sorted out to interpret the influence of the medium on the observed rate. The unified solvation model provides a means of sorting out these various contributions.

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 6009-70-7, in my other articles. Recommanded Product: 6009-70-7.

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

Synthetic Route of 629-25-4, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 629-25-4, Name is Sodium Laurate, SMILES is CCCCCCCCCCCC([O-])=O.[Na+], belongs to Benzisoxazole compound. In a article, author is LEE, JJ, introduce new discover of the category.

CATALYSIS OF DECARBOXYLATION OF 6-NITROBENZISOXAZOLE-3-CARBOXYLATE BY CATIONIC POLYMER COLLOIDS

Polystyrene latexes with quaternary ammonium ion-exchange sites catalyze the decarboxylation of 6-nitrobenzisoxazole-3-carboxylate in aqueous dispersions. A catalytic rate constant of 2.1 X 10(4) times the rate constant in water was achieved in particles containing 24 mol % of poly((styrylmethyl)tri-n-butylammonium chloride) repeat units. This is the largest rate enhancement reported at 25 degrees-C for decarboxylation of 6-nitrobenzisoxazole-3-carboxylate in any colloidal or polymeric medium. The decarboxylation kinetics fit both the enzyme model of micellar catalysis and an ion-exchange model. Added electrolyte decreases the rate of decarboxylation but increases the intrinsic catalytic rate constants in the more highly swollen latexes. The fraction of (styrylmethyl)trimethylammonium ion repeat units in the polymers has little effect on the rate of decarboxylation. The catalytic activity of the poly((styrylmethyl)trailkylammonium) ions in the latex increases in the order of in lipophilicity: Me < Et < Pr < Bu. The 200-350-nm diameter monodisperse colloidal particles with varied functional group content were prepared by emulsion copolymerization of styrene, (styrylmethyl)trimethylammonium chloride, divinylbenzene, and (chloromethyl)styrene followed by reactions with trialkylamines to form the anion-exchange sites. Synthetic Route of 629-25-4, 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 629-25-4 is helpful to your research.

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