Heterocyclic Building Blocks-Benzisoxazole

Having gained chemical understanding at molecular level, chemistry graduates may choose to apply this knowledge in almost unlimited ways, as it can be used to analyze all matter and therefore our entire environment, Formula: https://www.ambeed.com/products/35963-20-3.html.

A divergent and regioselective synthesis of either 3-substituted benzisoxazoles or 2-substituted benzoxazoles from readily accessible ortho-hydroxyaryl N-H ketimines is described. The reaction proceeds in two distinct pathways through a common N-Cl imine Intermediate: (a) N-O bond formation to form benzisoxazole under anhydrous conditions and (b) NaOCl mediated Beckmann-type rearrangement to form benzoxazole, respectively. The reaction path also depends on the electronic nature of the aromatic ring, with the electron-rich aromatic rings favoring the rearrangement and the electron-deficient rings favoring the N-O bond formation. A Beckmann-type rearrangement mechanism via net [1,2]-aryl migration for the formation of 2-substituted benzoxazole is proposed.

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

When developing chemical systems it’s of course important to gain a deep understanding of the chemical reaction process. 2836-32-0, Name is Sodium glycolate, SMILES is OCC([O-])=O.[Na+], in an article , author is Teslenko, Yuriy, once mentioned of 2836-32-0, Quality Control of Sodium glycolate.

The molecule of the title compound, C14H7Cl2NO2, is not planar; the dihedral angle between the mean planes of the chlorophenyl and benzisoxazole rings is 20.32 (7)degrees. The carbonyl chloride group is twisted with respect to the benzisoxazole ring by 2.5 (1)degrees. The molecular conformation is stabilized by an intramolecular C-H center dot center dot center dot Cl hydrogen bond. In the crystal packing, adjacent molecules are linked into dimers by intermolecular C-H center dot center dot center dot O hydrogen bonds. The dimers are further stacked into columns along the unique axis direction by pi-pi stacking interactions, with a centroid center dot center dot center dot centroid distance of 3.828 (5) angstrom. Other weak intermolecular C-H center dot center dot center dot O and C-H center dot center dot center dot Cl interactions are also present.

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

The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 6106-21-4, Name is Sodium succinate hexahydrate, SMILES is O=C([O-])CCC([O-])=O.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Na+].[Na+], in an article , author is Byrappa, Sathish, once mentioned of 6106-21-4, Synthetic Route of 6106-21-4.

Background: Triple Negative Breast Cancer (TNBC) tends to be more aggressive than other types of breast cancer. Resistance to chemotherapy is a major obstacle hence there is a significant need for new antineoplastic drugs with multi-target potency. Numerous Benzoisoxazole moieties have been found to possess a broad spectrum of pharmacological activities. In the present study, we have synthesized 9 novel derivatives of Benzisoxazole 7(a-i) and screened them for their biological potential. Methods: Chemical synthesis, Mass spectrometry (HRMS), cell proliferation and cytotoxicity assay, wound healing assay, flow cytometry and nuclear staining. Angio-inhibitory activity assessed by corneal micropocket assay and in vivo peritoneal angiogenesis assay. Results: The Benzisoxazole derivatives 7(a-i) were synthesized and screened for their biological potency by both in vitro and in vivo experimental models. Among the series, compound 3-(1-((3-(3(Benzyloxy)-4-methoxyphenyl)4,5-dihydroisoxazole-5-yl) methyl)piperidine-4-yl)6-fluorobenzo[d] isoxazole (7e) was found to be most promising, with an average IC50 value of 50.36 +/- 1.7 mu M in MTT assay and showed 81.3% cell death. The compound 7e also showed 60-70% inhibition on a recombinant Metastasis-Associated protein (MTA1) induced proliferation and cell migration in MDAMB-231 cells, which is known to play a major role in angiogenesis. The anti-tumour studies inferred the regression of tumour activity. This was due to inhibition of neovascularization and evoking apoptosis process as assessed by corneal vascularization, peritoneal angiogenesis and apoptotic hallmarks in 7e treated cells. Conclusion: These findings not only show the biological efficacy of compound 7e but it is also an effective beginning to explore the mechanism of metastasis and cancer therapy strategy targeting MTA1. The observed biological activity makes compound 7e an attractive drug candidate.

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

While the job of a research scientist varies, most chemistry careers in research are based in laboratories, where research is conducted by teams following scientific methods and standards.503-66-2, Name is 3-Hydroxypropionic Acid (contains varying amounts of 3,3-Oxydipropionic Acid), SMILES is O=C(O)CCO, in an article , author is Nenz, E, once mentioned of 503-66-2, Name: 3-Hydroxypropionic Acid (contains varying amounts of 3,3-Oxydipropionic Acid).

Interspecific somatic hybrid plants were obtained by symmetrical electrofusion of mesophyll protoplasts of Medicago sativa with callus protoplasts of Medicago arborea. Somatic hybrid calli were picked manually from semi-solid culture medium after they were identified by their dual color in fluorescent light. Twelve putative hybrid calli were selected and one of them regenerated plants. The morphogenesis of the somatic hybrid calli was induced by the synthetic growth regulator 1,2 benzisoxazole-3-acetic acid. Somatic hybrid plants showed intensive genome rearrangements, as evidenced by isozyme and RFLP analysis. The morphology of somatic hybrid plants was in general intermediate between the parents. The production of hybrids by protoplast fusion between sexually incompatible Medicago species is related to the in vitro responsiveness of the parental protoplasts. The possibility of using somatic hybrid plants in alfalfa breeding is discussed.

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

Having gained chemical understanding at molecular level, chemistry graduates may choose to apply this knowledge in almost unlimited ways, as it can be used to analyze all matter and therefore our entire environment, Electric Literature of 536-66-3.

Zonisamide is an orally administered antiepileptic drug that was first approved for clinical use in Japan in 1989. Since then, it has been licensed in Korea for a broad spectrum of epilepsies in adults and children, and in the USA for adjunctive therapy of adults with partial seizures, and in Europe for monotherapy of adults with newly diagnosed partial seizures and adjunctive therapy of adults and adolescents and children aged 6years with partial seizures with or without secondary generalization. Zonisamide is a benzisoxazole derivative with a unique chemical structure, predictable dose-dependent pharmacokinetics, and multiple complementary mechanisms of action. Treatment with zonisamide is well tolerated and is not known to be associated with clinically significant drug-drug interactions, including with oral contraceptives or other antiepileptic drugs. There have been >2million patient-years of experience with zonisamide for treatment of epilepsy, and this drug has International League Against Epilepsy level A evidence for efficacy/effectiveness as initial monotherapy for adults with partial-onset seizures. This review presents the evidence for zonisamide across the spectrum of epilepsy, with emphasis on real-world clinical practice and special populations of patients (children, elderly patients, and women of childbearing age) who are likely to be treated in daily clinical practice.

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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. 526-83-0, Name is 2,3-Dihydroxysuccinic acid, molecular formula is C4H6O6, Synthetic Route of 526-83-0, belongs to benzisoxazole compound, is a common compound. In a patnet, author is Chaker, Aida, once mentioned the new application about 526-83-0.

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

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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. Name: 4-(tert-Butoxy)-4-oxobutanoic acid, We very much hope you enjoy reading the articles and that you will join us to present your own research about 15026-17-2.

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

Chemical engineers work across a number of sectors, processes differ within each of these areas, but chemistry and chemical engineering roles are found throughout, and are directly involved in the manufacturing process of chemical products and materials. Name: 1,2-Bis(2-aminoethoxy)ethane.

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

Academic researchers, R&D teams, teachers, students, policy makers and the media all rely on us to share knowledge that is reliable, accurate and cutting-edge. 600-18-0, Name is 2-Oxobutanoic acid, formurla is C4H6O3. In a document, author is Kociolek, Martin G., introducing its new discovery. Application of 600-18-0.

A series of 2-hydroxyaryl ketoximes were converted to the corresponding 1,2-benzisoxazole 2-oxides by treatment with iodobenzene diacetate (in acetic acid or methanol) or N-chlorosuccinimide in water. Both methods gave moderate to excellent yields for a variety of substituted oximes under mild conditions within short reaction times. The latter method has the advantages of an aqueous solvent and lack of halogenated organic by-products.

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