28-Sep-21 News What Kind of Chemistry Facts Are We Going to Learn About C4H6O6

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DOES CHLORINATION MODIFY THE AUXIN-LIKE ACTIVITY OF 1,2-BENZISOXAZOLE-3-ACETIC ACID

The insertion of a chlorine atom in different positions of the aromatic ring did not increase the activity of benzisoxazole acetic acid, a new synthetic growth regulator, on shoot regeneration in vitro, pea stem elongation or flax root growth. This shows that this compound behaves differently from other synthetic auxins, and suggests that its activity is mainly related to the structure of its ring.

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

28-Sep News Interesting scientific research on C4H6O6

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THE METABOLISM AND EXCRETION OF RISPERIDONE AFTER ORAL-ADMINISTRATION IN RATS AND DOGS

The metabolism and excretion of risperidone (RIS; 3-[2-[4-(6-fluoro-1,2-benzisoxazole-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2- methyl-4H-pyrido[1,2-a]pyrimidin-4-one), a novel antipsychotic drug, were studied after single po administration of radiolabeled RIS to rats and dogs. In rats, the excretion of the radioactivity was very rapid. The predominant excretion in rat feces (78-82% of the dose) was related to an extensive biliary excretion of metabolites (72-79% of the dose), only a small part of which underwent enterohepatic circulation. In dogs, about 92% of the dose had been excreted after one week, and the fractions recovered in the urine and feces were comparable. Only a few percent of a po dose was excreted as unchanged RIS in rats as well as in dogs. Major metabolic pathways of RIS in rats and dogs were the same as those in humans. The main pathway was the hydroxylation at the alicyclic part of the 6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one moiety. The resulting 9-hydroxy-risperidone (9-OH-RIS) was the main metabolite in the excreta of dogs. In rats, the metabolism was more extensive, resulting in dihydroxy-RIS and hydroxy-keto Rls, which were eliminated mainly via the bile. However, in male and in female rats, just as in dogs and humans, the active metabolite 9-OH-RIS was by far the main plasma metabolite. Other major metabolic pathways were the oxidative dealkylation at the piperidine nitrogen and the scission of the isoxazole in the benzisoxazole ring system. The latter pathway appeared to be effected primarily by the intestinal microflora. The mass balance of the metabolites of RIS in dogs was dose independent from 0.05 to 1.25 mg/kg and was similar to that in humans.

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

26-Sep-21 News Final Thoughts on Chemistry for C4H6O6

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A PHARMACOLOGICAL, PHARMACOKINETIC AND CLINICAL OVERVIEW OF RISPERIDONE, A NEW ANTIPSYCHOTIC THAT BLOCKS SEROTONIN 5-HT2 AND DOPAMINE D-2 RECEPTORS

Risperidone is a benzisoxazole derivative with antipsychotic activity that is chemically unrelated to other currently available antipsychotic agents, Its neuropharmacological properties, characterized by potent central antagonism of both serotonin 5-HT2 and dopamine D-2 receptors, also differ from those of most other antipsychotic drugs, The pharmacokinetics of risperidone are well understood, having been studied in healthy subjects as well as in psychotic patients. The absolute oral bioavailability of risperidone is nearly 70%, and after oral administration, it is rapidly absorbed with the plasma level reaching a peak at about 1 h. 9-Hydroxyrisperidone, one of the metabolites of risperidone, is equally active with the parent compound and so the clinical activity of a dose of risperidone is due to the combined actions of both moieties, The plasma concentrations of risperidone and its active metabolite remain dose proportional even at doses exceeding the therapeutic range. In clinical trials with chronic schizophrenia patients, risperidone has an overall therapeutic activity comparable with that of haloperidol, but at doses that produce similar improvements in the positive symptoms of schizophrenia, risperidone has a greater effect on the negative symptoms and produces less extrapyramidal side effects than does haloperidol, However, additional controlled clinical studies are needed before the claims that risperidone is therapeutically superior to haloperidol cah be considered to be established firmly, Although risperidone is effective in acute schizophrenia and in non-treatment-resistant schizophrenics, studies adequately comparing risperidone with clozapine in treatment-resistant schizophrenic patients remain to be published. In addition, risperidone has been reported to be of value in patients with schizodepressive disorders, The clinical success of risperidone suggests that the development of compounds with selective affinity for 5-HT2 or other serotonin receptors may result in even further improvements in the pharmacotherapy of psychiatric disorders.

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

9/23/21 News Our Top Choice Compound: C4H6O6

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Modeling chemical reactions helps engineers virtually understand the chemistry, optimal size and design of the system, and how it interacts with other physics that may come into play. 526-83-0, Name is 2,3-Dihydroxysuccinic acid, SMILES is O=C(O)C(O)C(O)C(O)=O, in an article , author is Naveen, S., once mentioned of 526-83-0, SDS of cas: 526-83-0.

2-ethoxyphenyl)[4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl]methanone

In the title compound, C21H21FN2O3, the piperidine ring is in a chair conformation with the substituted benzisoxazole ring system in an equatorial position. An intermolecular C-H center dot center dot center dot O interaction is present in the crystal structure.

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

9/18/21 News The Best Chemistry compound: C4H6O6

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EXTRACTIVE SPECTROPHOTOMETRIC DETERMINATION OF QUETIAPINE FUMARATE IN PHARMACEUTICALS AND HUMAN URINE USING CALMAGITE AS AN ION-PAIR REAGENT

Quetiapine fumarate (QTF) is an antipsychotic drug belonging to the benzisoxazole derivatives indicated for the treatment of schizophrenia. A sensitive and selective method based on dichloromethane-extractable ion-pair of QTF with calmagite (CGT), which exhibited an absorption maximum at 490 nm, is described. At this. wavelength, Beer’s law is obeyed over the concentration range of 3.0-30.0 mu g ml(1). The apparent molar absorptivity, limit of detection (L OD) and quantitation (LOQ) values are 1.32×10(4) I mol(1) cm(-1), 0.27 and 0.81 mu g ml(1), respectively. The reaction is extremely rapid at room temperature and the absorbance values remain unchanged up to 19 h. The precision results, expressed as intra-day and inter-day relative standard deviation values, are satisfactory (RSD <= 2.2%). The accuracy is satisfactory as well (RE <= 2.44%). The method was successfully applied to the determination of QTF in pharmaceuticals and spiked human urine with satisfactory results. No interference was observed from common pharmaceutical adjuvants in tablets. Statistical comparison of the results with the official method showed an excellent agreement and indicated no significant difference in precision. Quality Control of 2,3-Dihydroxysuccinic acid, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 526-83-0.

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

9/18/21 News Extracurricular laboratory: Discover of C4H6O6

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An efficient synthesis of 3-chloromethyl-1,2-benzisoxazoles via modified Boekelheide rearrangement

An efficient and simple method for the preparation of 3-chloromethyl-1,2-benzisoxazoles by modified Boekelheide rearrangement using phosphorous oxychloride in moderate to good yields has been reported. The scope of the process in terms of synthetic utility and versatility is established.

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

16-Sep-21 News Extended knowledge of C4H6O6

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SYNTHESIS OF HETEROCYCLES FROM 4-(2-HYDROXYBENZOYL)-1-PHENYLPYRAZOLE

4-(2-Hydroxybenzoyl)-1-phenylpyrazole (1) has been used in the synthesis of benzofuran (2), coumarin (5) and benzisoxazole (9).

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

09/9/2021 News Awesome Chemistry Experiments For C4H6O6

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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

6 Sep 2021 News You Should Know Something about C4H6O6

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A facile preparation of 3-acyl-substituted isoxazolines, benzisoxazoles, and isoxazoles from the corresponding 3-carboxylate esters is described. The process, involving reaction of the ester derivative of 3-carboxylic acid substituted heterocycles with Grignard or alkynyl lithium reagents, leads to direct generation of the corresponding 3-acyl heterocycle. The presence of alpha-imino ester moieties in the heterocyclic substrates for the reactions is thought to be a key feature governing the nature of these transformations. The synthetic utility of the new methodology is demonstrated by its application in a two-step route for the preparation of novel linked bis-heterocycles. (C) 2012 Elsevier Ltd. All rights reserved.

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

2-Sep-2021 News Our Top Choice Compound: C4H6O6

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The emergence of multi-drug resistant pathogenic bacteria represents a serious and growing threat to national healthcare systems. Most pressing is an immediate need for the development of novel antibacterial agents to treat Gram-negative multi-drug resistant infections, including the opportunistic, hospital-derived pathogen, Acinetobacter baumannii. Herein we report a naturally occurring 1,2-benzisoxazole with minimum inhibitory concentrations as low as 6.25 mu g ml(-1) against clinical strains of multi-drug resistant A. baumannii and investigate its possible mechanisms of action. This molecule represents a new chemotype for antibacterial agents against A. baumannii and is easily accessed in two steps via de novo synthesis. In vitro testing of structural analogs suggest that the natural compound may already be optimized for activity against this pathogen. Our results demonstrate that supplementation of 4-hydroxybenzoate in minimal media was able to reverse 1,2-benzisoxazole’s antibacterial effects in A. baumannii. A search of metabolic pathways involving 4-hydroxybenzoate coupled with molecular modeling studies implicates two enzymes, chorismate pyruvate-lyase and 4-hydroxybenzoate octaprenyltransferase, as promising leads for the target of 3,6-dihydroxy-1,2-benzisoxazole.

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