Heterocyclic Building Blocks-Benzisoxazole

New discoveries in chemical research and development in 2021.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. 135236-72-5, Name is Calcium 3-hydroxy-3-methylbutanoate, SMILES is CC(C)(O)CC([O-])=O.CC(C)(O)CC([O-])=O.[Ca+2], in an article , author is Kitamura, S, once mentioned of 135236-72-5, Product Details of 135236-72-5.

Zonisamide (1,2-benzisoxazole-3-methanesulphonamide), a new anticonvulsant, is mainly metabolized to 2-sulphamoylacetylphenol by reduction of the benzisoxazole ring. Recent studies have shown that mammalian liver enzymes are responsible for the reduction of zonisamide. Because intestinal bacteria can also mediate the reduction of xenobiotics, this study was designed to evaluate the role of intestinal bacteria in in-vivo reductive metabolism of zonisamide. Treatment of rats with antibiotics significantly reduced the urinary and faecal excretion of 2-sulphamoylacetylphenol after oral administration of zonisamide. Re-contamination of the antibiotic-treated rats with microflora restored the excretion of the metabolite. The caecal contents of the control rats had significant zonisamide reductase activity, whereas little or no zonisamide reductase activity was observed with the caecal contents of the antibiotic-treated rats. Eight pure strains of intestinal bacteria were tested for zonisamide reductase activity and the highest was observed in Clostridium sporogenes. We concluded that intestinal bacteria play a major role in the reductive metabolism of zonisamide to 2-sulphamoylacetylphenol in-vivo.

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New discoveries in chemical research and development in 2021.SDS of cas: 123-99-9, 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. 123-99-9, Name is Water-soluble azelaic acid, molecular formula is C9H16O4. In an article, author is DUTTA, DK,once mentioned of 123-99-9.

ortho-Amino and N-alkylaminobenzophenones 3 have been prepared in good yields by the reductive cleavage of 2, 1-benzisoxazole and its salts with Zn-AlCl3.6H2O/THF system.

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 123-99-9 is helpful to your research. SDS of cas: 123-99-9.

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Benzisoxazole – Wikipedia,
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Chemical Research Letters, May 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. In an article, author is Younkin, Jason, once mentioned the application of 135236-72-5, Name is Calcium 3-hydroxy-3-methylbutanoate, molecular formula is C10H18CaO6, molecular weight is 274.32, MDL number is MFCD01318562, category is benzisoxazole. Now introduce a scientific discovery about this category, Quality Control of Calcium 3-hydroxy-3-methylbutanoate.

Several pharmacophore models have been proposed for 5-HT2A serotonin receptor antagonists. These typically consist of two aromatic/hydrophobic moieties separated by a given distance from each other, and from a basic amine. Although specified distances might vary, the models are relatively similar in their general construction. Because our preliminary data indicated that two aromatic (hydrophobic) moieties might not be required for such action, we deconstructed the serotonin-dopamine antipsychotic agent risperidone (1) into four smaller structural fragments that were thoroughly examined in 5-HT2A receptor binding and functional (i.e., two-electrode voltage clamp (TEVC) and intracellular calcium release) assays. It was apparent that truncated risperidone analogues behaved as antagonists. In particular, 6-fluoro-3-(1-methylpiperidin-4-yl)benzisoxazole (4) displayed high affinity for 5-HT2A, receptors (K-i, of ca. 12 nM) relative to risperidone (K-i of ca. 5 nM) and behaved as a potent 5-HT2A serotonin receptor antagonist. These results suggest that multiple aromatic (hydrophobic) moieties are not essential for high-affinity 5-HT2A receptor binding and antagonist activity and that current pharmacophore models for such agents are very much in need of revision.

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

New discoveries in chemical research and development in 2021.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. 536-66-3, Name is 4-Isopropylbenzoic acid, SMILES is C1=CC(=CC=C1C(C)C)C(O)=O, in an article , author is Steinhoff, B. J., once mentioned of 536-66-3, Formula: https://www.ambeed.com/products/536-66-3.html.

Zonisamide (ZNS) is a benzisoxazole derivate not structurally related to currently licensed antiepileptic drugs. It has multiple modes of action whose impact on the anticonvulsant effect is not yet fully understood: ZNS interrupts the synchronized neuronal firing through direct effects on voltage-dependent sodium and T-type calcium channels. Thus epileptiform propagation and activity are blocked. Furthermore ZNS has a modulating effect on the GABAergic inhibition, and may act on the dopaminergic and serotonergic neurotransmission and on acetylcholine pathways. An inhibition of excitatory glutamatergic transmission by reduction of the presynaptic release of glutamate has been also described. These modes of action suggest a broad anticonvulsant efficacy.

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Benzisoxazole – Wikipedia,
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Research speed reading in 2021. Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. Quality Control of Ammonium oxalate monohydrate, 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. 6009-70-7, Name is Ammonium oxalate monohydrate, molecular formula is C2H10N2O5. In an article, author is Nunes, Claudio M.,once mentioned of 6009-70-7.

UV irradiation of 3-amino-1,2-benzisoxazole isolated in an argon matrix leads to the formation of an amino-spiro-2H-azirine. The amino-spiro-2H-azirine was found to photoisomerize back to 3-amino1,2-benzisoxazole and also to a 1H-diazirine, which isomerizes to a carbodiimide. All the reported species were characterized experimentally by IR spectroscopy and confirmed by comparison with theoretical IR spectra. The discovery of the transformation of an amino-spiro-2H-azirine into a 1H-diazirine is unprecedented in the chemistry of reactive intermediates. (C) 2016 Elsevier Ltd. All rights reserved.

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

Chemical Research Letters, May 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. In an article, author is Falch, E, once mentioned the application of 35963-20-3, Name is ((1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid, molecular formula is C10H16O4S, molecular weight is 232.2966, MDL number is MFCD00064158, category is benzisoxazole. Now introduce a scientific discovery about this category, Application In Synthesis of ((1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid.

3-Methoxy-4,5,6,7-tetrahydro-1,2-benzisoxazol-4-one (20a), or the corresponding 3-ethoxy analogue (20b), and 3-chloro-4,5,6,7-tetrahydro-1,2-benzisothiazol-4-one (51) were synthesized by regioselective chromic acid oxidation of the respective bicyclic tetrahydrobenzenes 19a,b and 50, and they were used as key intermediates for the syntheses of the target; zwitterionic 3-isoxazolols 8-15 and 3-isothiazolols 16 and 17, respectively. These reaction sequences involved different reductive processes. Whereas (RS)-4-amino-3-hydroxy-4,5,6,7-tetrahydro-1,2-benzisoxazole (8, exo-THPO) was synthesized via aluminum amalgam reduction of oxime 22a or 22b, compounds 9,11-13, and 15-17 were obtained via reductive aminations. Compound 10 was synthesized via N-ethylation of the N-Boc-protected primary amine 25. The enantiomers of 8 were obtained in high enantiomeric purities (ee greater than or equal to 99.1%) via the diastereomeric amides 32 and 33, synthesized from the primary amine 23b and (R)-alpha-methoxyphenylacetyl chloride and subsequent separation by preparative HPLC. The enantiomers of 9 were prepared analogously from the secondary amine 27. On the basis of X-ray crystallographic analyses, the configuration of oxime 22a was shown to be E and the absolute configurations of (-)-8 . HCl and (+)-9 . HBr were established to be R. The effects of the target compounds on GABA uptake mechanisms in vitro were measured using a rat brain synaptosomal preparation and primary cultures of mouse cortical neurons and glia cells (astrocytes). Whereas the classical GABA uptake inhibitor, (R)-nipecotic acid (2), nonselectively inhibits neuronal (IC50 = 12 mu M) and glial (IC50 = 16 mu M) GABA uptake and 4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol (1, THPO) shows some selectivity for glial (IC50 = 268 mu M) versus neuronal (IC50 = 530 mu M) GABA uptake, exo-THPO (8) was shown to be more potent as an inhibitor of glial (IC50 = 200 mu M) rather than neuronal (IC50 = 900 mu M) GABA uptake. This selectivity was more pronounced for 9, which showed IC50 values of 40 and 500 mu M as an inhibitor of glial and neuronal GABA uptake, respectively. These effects of 8 and 9 proved to be enantioselective, (R)-(-)-8 and (R)-(+)-9 being the active inhibitors of both uptake systems. The selectivity of 9 as a glial GABA uptake inhibitor was largely lost by replacing the N-methyl group of 9 by an ethyl group, compound 10 being an almost equipotent inhibitor of glial (IC50 = 280 mu M) and neuronal (IC50 = 400 mu M) GABA uptake. The remaining target compounds, 11-17, were very weak or inactive as inhibitors of both uptake systems. Compounds 9-13 and 15 were shown to be essentially inactive against isoniazide-induced convulsions in mice after subcutaneous administration. The isomeric pivaloyloxymethyl derivatives of 9, compounds 43 and 44, were synthesized and tested as potential prodrugs in the isoniazide animal model. Both 43 (ED50 = 150 mu mol/kg) and 44 (ED50 = 220 mu mol/kg) showed anticonvulsant effects, and this effect of 43 was shown to reside in the (R)-(+)-enantiomer, 45 (ED50 = 44 mu mol/kg). Compound 9 also showed anticonvulsant activity when administered intracerebroventricularly (ED50 = 59 nmol).

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

New Advances in Chemical Research in 2021. Irreversible inhibitors are therefore the equivalent of poisons in heterogeneous catalysis. 505-48-6, Name is Octanedioic acid, molecular formula is C8H14O4, Product Details of 505-48-6, belongs to benzisoxazole compound, is a common compound. In a patnet, author is Caboni, E, once mentioned the new application about 505-48-6.

The effect of 1,2-benzisoxazole-3-acetic acid (BOA), compared to 1-naphthaleneacetic acid (NAA), on adventitious shoot formation in leaf portions acid compared to indolebutyric acid (IBA), on in vitro rooting in the apple (Malus domestica Borkh) cultivars McIntosh and Gals, and one rootstock, Jork 9, was investigated. BOA at 43.0 mu m or 2.7 mu m at NAA in combination with 17.8 mu m benzyladenine (BA), induced the highest number of explants to produce adventitious shoots in Jerk 9. In Gala, the combination of 21.5 mu m BOA with 1.0 mu m thidiazuron (TDZ) or with 22.0 mu m BA induced the highest regeneration percentages, 58 and 54%, respectively, giving more satisfactory results than NAA (where only 42% of leaf explants exhibited shoot formation). In McIntosh, the highest percentage of regeneration was obtained with 1.3 mu m NAA and 22.0 mu m BA, while 51% was the highest response obtained with the BOA treatment. The combination of BOA with TDZ completely inhibited regeneration activity in leaf portions of this cultivar. The shoots of all the genotypes obtained with the most morphogenetic NAA or BOA treatments were excised, multiplied and successfully rooted and hardened. The results demonstrate that the synthetic auxin BOA is active in inducing shoot regeneration from leaf explants of apple and that the activity of BOA in plant regeneration is genotype dependent. When BOA was used to induce rooting in apple microcuttings, lower rooting percentages were obtained than with IBA, showing that the effect of BOA in inducing root formation is very low and that it cannot be used routinely to replace IBA in the in vitro rooting of microcuttings.

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Benzisoxazole – Wikipedia,
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New Advances in Chemical Research in 2021. Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis, and research on the structure and performance of functional materials. 1113-38-8, Name is Ammonium oxalate, SMILES is O=C([O-])C([O-])=O.[NH4+].[NH4+], in an article , author is Banu, Afshan, once mentioned of 1113-38-8, COA of Formula: https://www.ambeed.com/products/1113-38-8.html.

In the title compound, C(18)H(11)BrN(4)OS, the imidazothiadiazole and benzisoxazole rings are individually planar with maximum deviations of 0.025 (3) 0.015 (4) angstrom, respectively, and are inclined at an angle of 23.51 (7)degrees with respect to each other. The planes of the imidazothiadiazole and bromophenyl rings are inclined at an angle of 27.34 (3)degrees. In the crystal, intermolecular C-H center dot center dot center dot N interactions result in chains of molecules along the b and c axes. Moreover, C-H center dot center dot center dot O interactions result in centrosymmetric head-to-head dimers with R(2)(2)(24) graph-set motifs. The molecular packing is further stabilized by pi-pi stacking interactions between the imidazole rings with a shortest centroid-centroid distance of 3.492 (3) angstrom. In addition, C-H center dot center dot center dot pi interactions are observed in the crystal structure.

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Chemical Research Letters, May 2021. In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. 503-66-2, Name is 3-Hydroxypropionic Acid (contains varying amounts of 3,3-Oxydipropionic Acid), molecular formula is C3H6O3, Application In Synthesis of 3-Hydroxypropionic Acid (contains varying amounts of 3,3-Oxydipropionic Acid), belongs to benzisoxazole compound, is a common compound. In a patnet, author is Dash, Radha Charan, once mentioned the new application about 503-66-2.

The dopamine D-2 receptor is involved in the etiology of a number of disorders, such as Parkinson’s disease, Huntington’s Chorea, tardive dyskinesia and schizophrenia. Antagonism of D-2 receptors is implicated in the treatment of various psychiatric disorders. In order to understand essential structural features required for D-2 antagonism, this research article elaborates on the generation of a four-point 3D pharmacophore model which was extracted from a series of 45 novel 3-[[(aryloxy)alkyl]piperidinyl]-1,2-benzisoxazole derivatives. The best pharmacophore model generated consisted of four PRRR features: a positively charged group (P), and three aromatic rings (R). Based on the model generated, a statistically valid 3D-QSAR with good predictability (Q(2) = 0.756) was derived. For the validation of the pharmacophore hypothesis, active compounds were docked against the 3D structure of the D-2 receptor which was constructed through homology modeling. Further, the derived pharmacophore was used as a query to search the Zinc ‘clean drug-like’ database. Hits retrieved were passed progressively through filters, such as fitness score, predicted activity and docking scores. The resulting hits present new scaffolds with a strong potential for D-2 antagonist.

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

New Advances in Chemical Research in 2021. Irreversible inhibitors are therefore the equivalent of poisons in heterogeneous catalysis. 68-04-2, Name is Sodium citrate, molecular formula is C6H5Na3O7, Quality Control of Sodium citrate, belongs to benzisoxazole compound, is a common compound. In a patnet, author is Shimoyama, R, once mentioned the new application about 68-04-2.

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. Quality Control of Sodium citrate.

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