Category: 57-11-4

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. 57-11-4, Name is Stearic acid, SMILES is CCCCCCCCCCCCCCCCCC(O)=O, in an article , author is Lalut, Julien, once mentioned of 57-11-4, SDS of cas: 57-11-4.

A rigidification strategy was applied to the preclinical candidate donecopride, an acetylcholinesterase inhibitor possessing 5-HT4R agonist activity. Inspired by promising bioactive benzisoxazole compounds, we have conducted a pharmacomodulation study to generate a novel series of multitarget directed ligands. The chemical synthesis of the ligand was optimized and compounds were evaluated in vitro against each target and in cellulo. Structure-activity relationship was supported by docking analysis in human acetylcholinesterase binding site. Among the synthesized compounds, we have identified a novel hybrid 32a (3-[2-[1-(cyclohexylmethyl)-4-piperidyl]ethyl]-4-methoxy-1,2-benzoxazole) able to display nanomolar acetylcholinesterase inhibitory effects and nanomolar Ki for 5-HT4R.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 57-11-4. SDS of cas: 57-11-4.

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

Research speed reading in 2021. Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 57-11-4, Name is Stearic acid, SMILES is CCCCCCCCCCCCCCCCCC(O)=O, in an article , author is Keles, Ergin, once mentioned of 57-11-4, Category: Benzisoxazole.

A simple colorimetric and fluorimetric chemosensor 3,5-dinitro-(N-phenyl)benzamide (DNBA), was synthesized for selective determination of cyanide anion in organic and aqueous solutions via novel chemodosimeter approach. The chemosensorDNBAshowed a chromogenic and fluorogenic selective response to CN(-)against competing anions such as F-, AcO-, and H(2)PO(4)(-)in organic (DMSO and ACN) and in aqueous solutions (in DMSO/H2O: 8:2, v/v). The intensive colorimetric and fluorimetric color changes were observed in ambient light and UV-light (lambda(ex). 365 nm) after cyanide interacted withDNBA. A method that can be used in the synthesis of new biologically active benzisoxazole compound was described by the reaction ofDNBAwith TBACN and KCN in DMSO or DMSO/H2O, respectively. All interaction mechanisms betweenDNBAand cyanide and fluoride anions were demonstrated by experimental studies using various spectroscopic methods such as UV/Vis, fluorescence,H-1/C-13 NMR, and mass spectrometry as well as X-ray diffraction method. In addition, the experimental results were also explained with theoretical data. The spectroscopic results showed that cyanide interacts with three different mechanisms; deprotonation, nucleophilic aromatic substitution, and formation of benzisoxazole ring.

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

New research progress on 57-11-4 in 2021. Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 57-11-4, Name is Stearic acid, SMILES is CCCCCCCCCCCCCCCCCC(O)=O, in an article , author is YOSHII, K, once mentioned of 57-11-4, Formula: https://www.ambeed.com/products/57-11-4.html.

The reaction of the silylated base of 1,2-benzisoxazol-3(2H)-one (1) and its 7-methyl derivative 5 and 5-methyl-1,2-benzisothiazol-3(2H)-one (9), respectively, with 1-O-acetyl-2,3,5-tri-O-benzoyl-beta-D-ribofuranose followed by basic deprotection gave the corresponding beta-D-ribonucleosides, and the silylated base of 1, when treated with 1-O-acetyl-2,3,5-tri-O-benzoyl-alpha-D-arabinofuranose in the presence of stannic chloride, afforded the corresponding alpha-arabinonucleoside. Structural proofs of these nucleosides are provided from elemental analyses and H-1 and C-13 nmr spectra.

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

Research speed reading in 2021. Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. Safety of Stearic acid, 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. 57-11-4, Name is Stearic acid, molecular formula is C18H36O2. In an article, author is MEWSHAW, RE,once mentioned of 57-11-4.

A series of 5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indoles and 6,7,8,9,10,11-hexahydro-7,-11-imino-5H-cyclooct[b]indoles was prepared. Structural modifications of the lead compound, 11-[4-(4-fluorobenzoyl)propyl]-5,6,7,8,9,10-hexahydro-7,10-iminocyclohept[b]indole (5, K(i) = 0.82 nM vs [H-3]ketanserin) enabled the identification of the functionality necessary for high affinity at serotonin 5-HT2 and dopamine D2 receptors in ligand binding studies. The indole ring, as well as the benzoyl or isosteric benzisoxazole moiety, were essential for high affinity. Variations of the length of the side chains resulted in ligands having either selective affinity for the 5-HT2 receptor or a combination of 5-HT2 and D2 affinity. In vivo binding studies were performed on selected members in this series. The most potent member, 2-fluoro-11-[4-(4-fluorobenzoyl)butyl]-5,6,7,8,9,-10-hexahydro-7,10-iminocyclohept[b]indole (36) had an ED50 of <1 mg/kg at the 5-HT2 and D2 receptors following oral administration. 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 57-11-4, in my other articles. Safety of Stearic acid.

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

Research speed reading in 2021. Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. HPLC of Formula: https://www.ambeed.com/products/57-11-4.html, 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. 57-11-4, Name is Stearic acid, molecular formula is C18H36O2. In an article, author is Umamaheswari, J.,once mentioned of 57-11-4.

The present study deals with the synthesis of benzisoxazole derivatives beginning from 5,5-dimethyl cyclohexane-1,3-dione by making use of a microwave reactor. The microwave reactions are effortless, well-organized, clean, swift and financially viable for the synthesis of a huge amount of organic molecules, have offered the drive for many chemists to change from conventional heating methods to microwave-assisted chemistry. In latest years, microwave synthesized organic reaction has appeared as a new device in organic synthesis. The synthesized compounds were for the studie by using IR, NMR, mass spectra and antimicrobial studies also carried out.

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

Chemical Research Letters, May 2021. In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. 57-11-4, Name is Stearic acid, molecular formula is C18H36O2, Computed Properties of https://www.ambeed.com/products/57-11-4.html, belongs to benzisoxazole compound, is a common compound. In a patnet, author is Basarab, Gregory S., once mentioned the new application about 57-11-4.

The compounds described herein with a spirocyclic architecture fused to a benzisoxazole ring represent a new class of antibacterial agents that operate by inhibition of DNA gyrase as corroborated in an enzyme assay and by the inhibition of precursor thymidine into DNA during cell growth. Activity resided in the configurationally lowest energy (2S,4R,4aR) diastereomer. Highly active compounds against Staphylococcus aureus had sufficiently high solubility, high plasma protein free fraction, and favorable pharmacokinetics to suggest that in vivo efficacy could be demonstrated, which was realized with compound (-)-1 in S. aureus mouse infection models. A high drug exposure NOEL on oral dosing in the rat suggested that a high therapeutic margin could be achieved. Importantly, (-)-1 was not cross-resistant with other DNA gyrase inhibitors such as fluoroquinolone and aminocoumarin antibacterials. Hence, this class shows considerable promise for the treatment of infections caused by multidrug resistant bacteria, including S. aureus.

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Reference:
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. 57-11-4, Name is Stearic acid, SMILES is CCCCCCCCCCCCCCCCCC(O)=O, in an article , author is Kitamura, S, once mentioned of 57-11-4, Application In Synthesis of Stearic acid.

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

New Advances in Chemical Research in 2021. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. 57-11-4, Name is Stearic acid, SMILES is CCCCCCCCCCCCCCCCCC(O)=O, in an article , author is Hoy, Sheridan M., once mentioned of 57-11-4, Quality Control of Stearic acid.

Oral zonisamide (Zonegran(A (R))) is a benzisoxazole derivative chemically unrelated to other antiepileptic drugs (AEDs). It is approved in the EU as an adjunct to other AEDs in the treatment of pediatric patients aged a parts per thousand yen6 years with partial seizures, with or without secondary generalization. In a randomized, double-blind, multinational, phase III study in pediatric patients aged 6-17 years with partial seizures, the proportion of patients achieving a a parts per thousand yen50 % reduction from baseline in seizure frequency per 28 days during the maintenance treatment period was significantly higher with adjunctive therapy with zonisamide than placebo. The antiepileptic efficacy of zonisamide was sustained during a 59-week extension study in this patient population. Zonisamide was generally well tolerated in these studies, with the majority of adverse events being mild or moderate in severity. Thus, oral zonisamide as an adjunctive therapy to other AEDs provides a useful option in the treatment of pediatric patients aged a parts per thousand yen6 years with partial seizures.

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

In an article, author is Hoy, Sheridan M., once mentioned the application of 57-11-4, Name: Stearic acid, Name is Stearic acid, molecular formula is C18H36O2, molecular weight is 284.4773, MDL number is MFCD00002752, category is benzisoxazole. Now introduce a scientific discovery about this category.

Zonisamide: A Review of Its Use as Adjunctive Therapy in the Management of Partial Seizures in Pediatric Patients Aged >= 6 Years

Oral zonisamide (Zonegran(A (R))) is a benzisoxazole derivative chemically unrelated to other antiepileptic drugs (AEDs). It is approved in the EU as an adjunct to other AEDs in the treatment of pediatric patients aged a parts per thousand yen6 years with partial seizures, with or without secondary generalization. In a randomized, double-blind, multinational, phase III study in pediatric patients aged 6-17 years with partial seizures, the proportion of patients achieving a a parts per thousand yen50 % reduction from baseline in seizure frequency per 28 days during the maintenance treatment period was significantly higher with adjunctive therapy with zonisamide than placebo. The antiepileptic efficacy of zonisamide was sustained during a 59-week extension study in this patient population. Zonisamide was generally well tolerated in these studies, with the majority of adverse events being mild or moderate in severity. Thus, oral zonisamide as an adjunctive therapy to other AEDs provides a useful option in the treatment of pediatric patients aged a parts per thousand yen6 years with partial seizures.

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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, 57-11-4, Name is Stearic acid, SMILES is CCCCCCCCCCCCCCCCCC(O)=O, in an article , author is Karandikar, Shubhendu, once mentioned of 57-11-4, Category: Benzisoxazole.

1,2-Benzisoxazole-3-acetamide derivatives as dual agents for DPP-IV inhibition and anticancer activity

Herein, we have designed various benzisoxazole acetamide derivatives with and without glycine spacer as DPP-IV inhibitors. Compounds 9a-d and 11a-e were synthesized and screened for their in vitro DPP-IV inhibition. Compounds 11a and 11c showed moderate activity for DPP-IV inhibition, whereas other remained inactive at 25-200 mu M concentrations. DPP-IV inhibition can be a good strategy for modulating diabetes and cancer; hence, we have screened compounds 9a-d and 11a-e for their anticancer activity using MTT assay against A549 and MCF7 cell lines. Compounds 9a-d without glycine spacer have shown good anticancer activity compared to compounds 11a-e with glycine spacer. Compound 9b has shown moderate activity with IC50 values 4.72 +/- 0.72 and 4.39 +/- 0.809 mu M against A549 and MCF7 cell lines, respectively. Interestingly, compound 9c with cyano group has shown very good anticancer activity with IC50 2.36 +/- 0.34 mu M against MCF7 cell line as compared to fluorouracil with IC50 45.04 +/- 1.02 mu M. [GRAPHICS] .

Interested yet? Read on for other articles about 57-11-4, you can contact me at any time and look forward to more communication. Category: Benzisoxazole.

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