Heterocyclic Building Blocks-Benzisoxazole

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 68-04-2, Name is Sodium citrate, SMILES is O=C(CC(C([O-])=O)(O)CC([O-])=O)[O-].[Na+].[Na+].[Na+], belongs to Benzisoxazole compound. In a document, author is Shimoyama, R, introduce the new discover, Safety of Sodium citrate.

Monitoring of zonisamide in human breast milk and maternal plasma by solid-phase extraction HPLC method

An HPLC method was developed for the determination of zonisamide in human breast milk and plasma. Chromatographic separation was achieved using a Develosil CN analytical column with potassium dihydrogenphosphate buffer (pH 3.5 with milk, pH 2.5 with plasma)-acetonitrile as the mobile phase. Zonisamide and 1,2-benzisoxazole-3-methansulfonamine acetate as internal standard were detected by ultraviolet absorbance at 240 nm. Zonisamide in breast milk and plasma was extracted by a rapid and simple procedure based on C-18 bonded-phase extraction. Determination of zonisamide in human breast milk and plasma was possible in the concentration range 0.05-20.0 mu g/mL. The recoveries of zonisamide added to human breast milk and plasma were 79.5-85.0% and 86.3-93.1%, respectively, with coefficients of variation of less than 8.3% and 11.4% respectively. The mean concentrations of zonisamide in breast milk and plasma were 9.41 +/- 0.95 and 10.13 +/- 0.45 mu g/mL, respectively. The average ratio between the breast milk concentration and plasma concentration (M/P ratio) was 0.93 +/- 0.09. Copyright (C) 1999 John Wiley & Sons, Ltd.

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 68-04-2 is helpful to your research. Safety of Sodium citrate.

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

Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage and in condensed media, causing turnover rates to depend strongly on interfacial structure and composition, 6009-70-7, Name is Ammonium oxalate monohydrate, SMILES is O=C([O-])C([O-])=O.[H]O[H].[NH4+].[NH4+], in an article , author is Sakuma, Shogo, once mentioned of 6009-70-7, Computed Properties of C2H10N2O5.

High-Density Lipoprotein Cholesterol-Elevating Effect of a Novel Peroxisome Proliferator-Activated Receptor delta Agonist

We report the synthesis and evaluation of a novel PPAR delta agonist, compound 12a, characterized by a benzisoxazole ring. Compound 12a exhibited a potent human PPAR delta transactivation activity (EC50: 0.011 mu M). Preliminary biological testing suggests that compound 12a has significant HDL-cholesterol elevating effect in an animal model of dyslipidemia.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 6009-70-7, you can contact me at any time and look forward to more communication. Computed Properties of C2H10N2O5.

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

Synthetic Route of 133-37-9, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 133-37-9, Name is (2R,3R)-rel-2,3-Dihydroxysuccinic acid, SMILES is O=C(O)[C@H](O)[C@@H](O)C(O)=O, belongs to Benzisoxazole compound. In a article, author is Aitipamula, Srinivasulu, introduce new discover of the category.

Cocrystals of zonisamide: physicochemical characterization and sustained release solid forms

We report four cocrystals of the antiepileptic drug, zonisamide (ZNS), which encounters half-life fluctuation when administered adjunctly with other antiepileptic drugs. Single crystals for two of the novel cocrystals of ZNS were successfully prepared from solvent evaporation experiments and their crystal structures were determined. Pharmaceutically acceptable cocrystals were analyzed for their dissolution rate, solubility and stability to draw conclusions on the impact of cocrystallization on the physicochemical properties of ZNS. It was found that the cocrystals showed lower solubility and dissolution rates and offer potential benefits in the development of sustained release formulations of ZNS which could address issues regarding its half-life fluctuation. Recent attempts to explore newer therapeutic applications have suggested ZNS as a potential drug for weight loss management. In this regard, the cocrystal of ZNS with caffeine, which has also been used in weight loss management, promises potential applications in the development of a novel fixed-dose combination drug which could offer synergistic therapeutic benefits in the treatment of obesity.

Synthetic Route of 133-37-9, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 133-37-9.

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. , Category: Benzisoxazole, 636-61-3, Name is (R)-2-Hydroxysuccinic acid, molecular formula is C4H6O5, belongs to Benzisoxazole compound. In a document, author is MUTLIB, AE, introduce the new discover.

APPLICATION OF HYPHENATED LC/NMR AND LC/MS TECHNIQUES IN RAPID IDENTIFICATION OF IN-VITRO AND IN-VIVO METABOLITES OF ILOPERIDONE

Iloperidone, 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl]-1-piperidinyl]propoxy]-3-methoxyphenyl]ethanone, is currently undergoing clinical trials as a potential antipsychotic agent. Iloperidone was found to be extensively metabolized to a number of metabolites by rats, dogs, and humans, LC/MS/MS was used to characterize and identify metabolites of iloperidone present in complex biological mixtures obtained from all three species. Identification of some of the unknown metabolites in rat bile was achieved successfully by combination of LC/NMR and LC/MS with a minimum amount of sample cleanup. The utility of coupling a semipreparative HPLC to LC/MS instrument for further characterization of collected metabolites was demonstrated. It was shown that iloperidone was metabolized by O-dealkylation processes to yield 6-fluoro-3-[1-[3-hydroxypropyl)-4-piperidinyl]-1,2-benzisoxazole and 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-2-hydroxyphenyl]ethanone. Oxidative N-dealkylation led to the formation of 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole and a secondary metabolite, 3-[(4-acetyl-2-methoxy)phenoxy]propionic acid. Iloperidone was reduced to produce 4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxy-alpha-methylbenzenemethanol as the major metabolite in humans and rats. Hydroxylation of iloperidone produced 1-[4-[3-[4-(6-fluoro-1 ,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-2-hydroxy-5-methoxyphenyl]ethanone and 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1 -piperidinyl]-3-methoxyphenyl]propoxy]-2-hydroxyethanone, the later of which was found to be the principal metabolite in dogs. The identities of all these metabolites were established by comparing the LC/MS retention times and mass spectral data with synthetic standards.

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 636-61-3. Category: Benzisoxazole.

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. 427-49-6, Name is alpha-Cyclopentylmandelic Acid, formurla is C13H16O3. In a document, author is Chaker, Aida, introducing its new discovery. Product Details of 427-49-6.

New 3-substituted-2,1-benzisoxazoles: Synthesis and antimicrobial activities

A new series of 3-substituted-2,1-benzisoxazoles (anthranils) were prepared by different methods and characterized by spectroscopic methods and mass spectrometry. These 2,1-benzisoxazoles were tested in vitro for their antiplasmodial activity on a chloroquine-resistant strain of Plasmodium falciparum (P.f.) (FcB1), and for antimicrobial activity against representative bacterial and fungal strains, as well as for cytotoxicity on MCF7 human breast cancer cells. Given the log P-calc and selectivity index values (cytotoxicity/antiplasmodial activity ratio), the benzo[c] isoxazol-3- ylmethylene-phenyl-amine (11) (imino-benzisoxazole) was identified as the best hit against P.f. (FcB1), and the benzo[c] isoxazol-3-yl-phenyl-methanone (3) (3-acyl-2,1-benzisoxazole) against P.f. and the Geotrichum candidum fungal strain. (c) 2013 Production and hosting by Elsevier B.V. on behalf of King Saud University.

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

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, Application In Synthesis of Sodium benzoate, 532-32-1, Name is Sodium benzoate, SMILES is O=C([O-])C1=CC=CC=C1.[Na+], belongs to Benzisoxazole compound. In a document, author is Brown-Proctor, C, introduce the new discover.

Synthesis and evaluation of 6-[C-11]methoxy-3-[2-[l-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole as an in vivo radioligand for acetylcholinesterase

6-Methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole is a high affinity (K-i = 8.2 nM) reversible inhibitor of acetylcholinesterase (AChE). The carbon-11 labeled form was prepared in high (>97%) radiochemical purity and with specific activities of 37 +/- 20 GBq/mu mol at end of synthesis, by the alkylation of the desmethyl precursor with [C-11]methyl trifluoromethanesulfonate in N,N dimethylformamide at room temperature. In vivo studies in mice demonstrated good blood brain permeability but essentially uniform regional brain distribution. Thus, despite in vitro and in vivo activity as an AChE inhibitor, 6-[C-11]methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole does not appear to be a good candidate for in vivo imaging studies of AChE in the mammalian brain. NUCL MED BIOL 26;1: 99-103, 1999. (C) 1999 Elsevier Science Inc.

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 532-32-1 is helpful to your research. Application In Synthesis of Sodium benzoate.

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. , HPLC of Formula: C13H8ClNO, 719-64-2, Name is 5-Chloro-3-phenylbenzo[c]isoxazole, molecular formula is C13H8ClNO, belongs to Benzisoxazole compound. In a document, author is Arava, Veera Reddy, introduce the new discover.

Novel base catalysed rearrangement of sultone oximes to 1,2-benzisoxazole-3-methane sulfonate derivatives

A new process for the preparation of 1,2-benzisoxazole-3-methanesulfonates and 4-oximino-2,3dihydrobenzoxathiin- 2,2-dioxides (sultone oximes) is described. These compounds are important intermediates for the preparation of zonisamide, an anti-convulsant drug.

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 719-64-2. HPLC of Formula: C13H8ClNO.

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

Electric Literature of 40052-13-9, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 40052-13-9, Name is 3-Tert-butoxy-3-oxopropanoic acid, SMILES is CC(C)(C)OC(=O)CC(O)=O, belongs to Benzisoxazole compound. In a article, author is Jain, M, introduce new discover of the category.

1,2-benzisoxazole phosphorodiamidates as novel anticancer prodrugs requiring bioreductive activation

Several 1,2-benzisoxazole phosphorodiamidates have been designed as prodrugs of phosphoramide mustard requiring bioreductive activation. Enzymatic reduction of 1,2-benziosoxazole moiety is expected to result in the formation of imine intermediate due to the cleavage of the N-O bond. The imine should then be spontaneously hydrolyzed to a ketone metabolite, thereby facilitating base-catalyzed beta-elimination of cytotoxic phosphoramide mustard. As expected, the proposed prodrugs 4, 9, and 12 were at least 3-5-fold more potent cytotoxins than control compounds 5 and 15, which lack in the phosphoramide mustard group. Upon incubation with phenobarb-induced rat liver S-9 fraction, compounds 4, 9, and 12 underwent extensive NADPH-dependent metabolism with concomitant generation of alkylating activity under both hypoxic and oxic conditions. Corresponding ketone metabolites were detected for 9 and 15. NADPH-dependent bioreduction of 15 to its ketone metabolite 16 was located in the microsomal fraction and inhibited by SKF-525A and pCMBA. Compared with phenobarb-induced rat liver microsomal fraction, incubation of 15 with rat or human P450 reductase microsomes showed moderate generation of 16. Microsomal cytochrome P450 and/or P450 reductase appear to be involved in the reductive metabolism of 1,2-benzisoxazole moiety under hypoxic as well as oxic conditions.

Electric Literature of 40052-13-9, 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 40052-13-9 is helpful to your research.

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. 99189-60-3, Name is 2-[1-(2-Amino-2-oxoethyl)cyclohexyl]acetic Acid, formurla is C10H17NO3. In a document, author is Gentile, Salvatore, introducing its new discovery. Name: 2-[1-(2-Amino-2-oxoethyl)cyclohexyl]acetic Acid.

A systematic review of quality of life and weight gain-related issues in patients treated for severe and persistent mental disorders: focus on aripiprazole

Aripiprazole is a relatively novel second-generation antipsychotic belonging to the chemical class of benzisoxazole derivatives and is characterized by a unique pharmacological profile which suggests that the drug acts as a dopamine-serotonin system stabilizer. Whereas all previously available antipsychotics are antagonists at D-2 receptors, aripiprazole is the only available partial agonist at these receptors. Thus, it has been suggested that aripiprazole could be associated with a relatively neutral impact on bodyweight, possibly reducing risks of a detrimental impact on the quality of life that often complicates management for a large number of patients diagnosed with severe and persistent mental disorders (SPMDs) treated chronically with antipsychotic medications. However, data from short- and long-term reviewed studies indicate that the prevalence rate of clinically relevant weight gain during therapy with this drug is similar to that occurring during treatments with other antipsychotic agents, either typical or atypical. Moreover, information on the impact of aripiprazole therapy on the quality of life of patients diagnosed with SPMDs is scarce and characterized by conflicting results. Given these results, further, large, well-designed studies are needed before confirming potential advantages of aripiprazole over first-generation antipsychotics and other SGAs.

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 99189-60-3 help many people in the next few years. Name: 2-[1-(2-Amino-2-oxoethyl)cyclohexyl]acetic Acid.

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

Synthetic Route of 503-74-2, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 503-74-2, Name is 3-Methylbutanoic acid, SMILES is CC(C)CC(O)=O, belongs to Benzisoxazole compound. In a article, author is Mikhailovskii, A. G., introduce new discover of the category.

2-AROYLHEXANONES IN THE SYNTHESIS OF AZOLES

2-Aroylcyclohexanones, obtained from piperidinocyclohexene, react with hydrazine, hydroxylamine, and o-phenylenediamine to give the corresponding derivatives of bicyclic heterocycles – indazole, 2,1-benzisoxazole, and 2-spiro-cyclohexylbenzimidazole. The structure of a derivative of benzyloxazole has been determined by X-ray crystallography.

Synthetic Route of 503-74-2, 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 503-74-2 is helpful to your research.

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