Tag: M.W:200-300

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 57-11-4, Name is Stearic acid, molecular formula is C18H36O2. In an article, author is Kitamura, S,once mentioned of 57-11-4, Safety of Stearic acid.

The role of mammalian intestinal bacteria in the reductive metabolism of zonisamide

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.

Interested yet? Keep reading other articles of 57-11-4, you can contact me at any time and look forward to more communication. Safety of Stearic acid.

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

Reference of 35963-20-3, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 35963-20-3, Name is ((1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid, SMILES is O=S(C[C@]1(C2(C)C)C(C[C@]2([H])CC1)=O)(O)=O, belongs to benzisoxazole compound. In a article, author is White, HS, introduce new discover of the category.

Correlation between anticonvulsant activity and inhibitory action on glial gamma-aminobutyric acid uptake of the highly selective mouse gamma-aminobutyric acid transporter 1 inhibitor 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and its N-alkylated analogs

The inhibitory effect of 3-hydroxy-4-amino-4,5,6,7-tetrahydro1,2-benzisoxazole (exo-THPO) and its N-methylated (N-methylexo-THPO) and N-ethylated (N-ethyl-exo-THPO) analogs, derived from gamma-aminobutyric acid (GABA) and 4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol (THPO) on GABA transport was investigated using cultured neocortical neurons (GABAergic) and astrocytes and cloned mouse GABA transporters GAT1-4 expressed in human embryonic kidney (HEK) 293 cells. Anticonvulsant activity was assessed after i.c.v. administration to Frings audiogenic seizure-susceptible mice. Anticonvulsant activity of the O-pivaloyloxymethyl prodrug of N-methyl-exo-THPO was assessed after i.p. administration. Results from these studies were compared with those obtained from similar studies with the novel anticonvulsant drug tiagabine, which acts via inhibition of GABA transport. exo-THPO and its N-alkyl analogs inhibited neuronal, astrocytic, and GAT1-mediated GABA transport but not GABA uptake mediated by GAT2-4. N-Methyl-exo-THPO was 8-fold more potent as an inhibitor of astrocytic versus neuronal GABA uptake. The IC50 value for inhibition of GABA uptake by GAT1 closely reflected its IC50 value for inhibition of neuronal uptake. Tiagabine was approximately 1000-fold more potent than exoTHPO and its alkyl derivatives as an inhibitor of GABA uptake in cultured neural cells and GAT1-expressing HEK 293 cells. exoTHPO, its alkylated analogs, and tiagabine displayed a time- and dose-dependent inhibition of audiogenic seizures after i.c.v. administration. N-Methyl-exo-THPO was the most potent anticonvulsant among the exo-THPO compounds tested and only slightly less potent than tiagabine. The findings suggest a correlation between anticonvulsant efficacy and selective inhibition of astroglial GABA uptake. Furthermore, results obtained with the N-methyl-exo-THPO prodrug demonstrate the feasibility of developing a glial-selective GABA uptake inhibitor with systemic bioavailability.

Reference of 35963-20-3, 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 35963-20-3 is helpful to your research.

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

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Name: alpha-Cyclopentylmandelic Acid, 427-49-6, Name is alpha-Cyclopentylmandelic Acid, SMILES is O=C(O)C(O)(C1CCCC1)C2=CC=CC=C2, in an article , author is Murai, Kenichi, once mentioned of 427-49-6.

Reactivity of the ester group attached isoxazoline, benzisoxazole, and isoxazole: a facial preparation of 3-acyl-substituted these heterocycles

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.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 427-49-6, you can contact me at any time and look forward to more communication. Name: alpha-Cyclopentylmandelic Acid.

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

Application of 6106-21-4, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 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+], belongs to benzisoxazole compound. In a article, author is Panza, Francesco, introduce new discover of the category.

Pharmacological management of dementia with Lewy bodies with a focus on zonisamide for treating parkinsonism

Introduction Dementia with Lewy bodies (DLB) has no approved symptomatic or disease-modifying treatments in the US and Europe, despite being the second most common cause of neurodegenerative dementia. Areas covered Herein, the authors briefly review the DLB drug development pipeline, providing a summary of the current pharmacological intervention studies. They then focus on the anticonvulsant zonisamide, a benzisoxazole derivative with a sulfonamide group and look at its value for treating parkinsonism in DLB. Expert opinion Several new compounds are being tested in DLB, the most innovative being those aimed at decreasing brain accumulation of alpha-synuclein. Unfortunately, new drug testing is challenging in terms of consistent diagnostic criteria and lack of reliable biomarkers. Few randomized controlled trials (RCTs) are well-designed, with enough power to detect significant drug effects. Levodopa monotherapy can treat the parkinsonism in DLB, but it can cause agitation or visual hallucination worsening. Two Phase II/III RCTs of DLB patients recently reported a statistically significant improvement in motor function in those receiving zonisamide as an adjunctive treatment to levodopa. New biomarker strategies and validated outcome measures for DLB or prodromal DLB may enhance clinical trial design for the development of specific disease-modifying treatments.

Application of 6106-21-4, 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 6106-21-4 is helpful to your research.

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

Chemistry is an experimental science, Product Details of 719-64-2, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 719-64-2, Name is 5-Chloro-3-phenylbenzo[c]isoxazole, molecular formula is C13H8ClNO, belongs to benzisoxazole compound. In a document, author is Hamada, K.

Contrasting effects of zonisamide and acetazolamide on amygdaloid kindling in rats

Purpose: Zonisamide (ZNS) and acetazolamide (AZM) are two antiepileptic drugs (AEDs) that differ in clinical efficacy. To elucidate the mechanisms of action of these compounds, we investigated their therapeutic and prophylactic effects in rats by using a kindling model of partial epilepsy. Methods: Electrodes were implanted into the left amygdala of adult male Wistar rats. The animals were stimulated at the afterdischarge threshold until Five stage 5 seizures were induced. The generalized seizure threshold was then determined. Therapeutic effects were examined in rats manifesting successive convulsions with near-threshold stimulation. To test prophylactic effects, drugs were administered intraperitoneally before daily kindling stimulation until the animal had a stage 5 seizure or reached day 18. Results: ZNS (10-40 mg/kg; n = 6) suppressed kindled seizures in a dose-dependent manner. Repeated administration for 7 days produced tolerance to anticonvulsive effects. AZM (25-200 mg/kg; n = 7) showed limited therapeutic effect, alleviating only the clonic convulsion in stage 5 seizures and reducing afterdischarge duration. Secondary generalization was not significantly suppressed during repeated treatment (50-200 mg/kg; n = 6). ZNS, 25 or 40 mg/kg (n = 8), significantly retarded seizure development; 15.0 or 17.0 daily stimulations were required to produce a stage 5 seizure. AZM, 50-200 mg/ kg (n = 6), also retarded seizure development, with 14.0-14.8 stimulations required. Conclusions: ZNS exhibited modest therapeutic and prophylactic effects, whereas AZM showed mainly prophylactic effects. Hypotheses are presented that may explain the mechanisms of action of these drugs.

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 719-64-2, in my other articles. Product Details of 719-64-2.

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

4246-51-9, Name is 3,3′-((Oxybis(ethane-2,1-diyl))bis(oxy))bis(propan-1-amine), molecular formula is C10H24N2O3, belongs to benzisoxazole compound, is a common compound. In a patnet, author is Sergeeva, MV, once mentioned the new application about 4246-51-9, COA of Formula: C10H24N2O3.

Hapten design for antibody-catalyzed decarboxylation and ring-opening reactions of benzisoxazoles

Three benzisoxazole haptens designed to elicit antibody binding sites with widely differing polarity have been synthesized and used to induce antibodies in mice. Monoclonal antibodies were prepared using hybridoma technology, and screened for catalysis of the ring-opening isomerization and/or decarboxylation of a series of related benzisoxazoles and their 3-carboxy-derivatives. No catalysis of decarboxylation was observed, but 3 of a total of 47 antibodies obtained against the three haptens catalyzed the isomerization process. Of 12 antibodies raised against the 3-acetylbenzisoxazole structure 5 none was catalytically active; but one of 24 raised against a 3-isopropenylbenzisoxazole 6 increased the rate of ring-opening of 6-nitrobenzisoxazole, and 5 of 11 antibodies raised against a benzisoxazole 7 with a 3-amidinium group were moderately active against either 6-nitro or 6-acylaminobenzisoxazoles. Competitive binding studies suggest that at least some of the antibodies induced by the isopropenyl hapten do possess a recognizably hydrophobic binding site.

If you’re interested in learning more about 4246-51-9. The above is the message from the blog manager. COA of Formula: C10H24N2O3.

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

Let’s face it, organic chemistry can seem difficult to learn. Especially from a beginner’s point of view. Like 57-11-4, Name is Stearic acid. In a document, author is De Simone, G, introducing its new discovery. Product Details of 57-11-4.

Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studies

The antiepileptic drug zonisamide was considered to act as a weak inhibitor of the zinc enzyme carbonic anhydrase (CA, EC 4.2. 1.1) (with a K, of 4.3 mu M against the cytosolic isozyme 11). Here we prove that this is not true. Indeed, testing zonisamide in the classical assay conditions of the CO2 hydrase activity of hCA II, with incubation times of enzyme and inhibitor solution of 15 min, a K-1 of 10.3 mu M has been obtained. However, when the incubation between enzyme and inhibitor was prolonged to 1d h, the obtained K-1 was of 35.2 nM, of the same order of magnitude as that of the clinically used sulfonamides/sulfamates acetazolantide, methazolamide, ethoxzolamide and topiramate (K(1)s in the range of 5.4-15.4 nM). The inhibition of the human mitochondrial isozyme hCA V with these compounds has been also tested by means of a dansylamide competition binding assay, which showed zonisamide and topiramate to be effective inhibitors, with K(1)s in the range of 20.6-25.4 nM. The X-ray crystal structure of the adduct of hCA 11 with zonisamide has also been solved at a resolution of 1.70 A, showing that the sulfonamide moiety participates in the classical interactions with the Zn(II) ion and the residues Thr199 and Glu106, whereas the benzisoxazole ring, is oriented toward the hydrophobic half of the active site, establishing a large number of strong van der Waals interactions (< 4.5 A) with residues Gln92, Vall2l, Phe131, Leu198, Thr200, Pro202. (c) 2005 Elsevier Ltd. All rights reserved. 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 57-11-4 help many people in the next few years. Product Details of 57-11-4.

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

Electric Literature of 57-11-4, 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, belongs to benzisoxazole compound. In a article, author is Sano, Hiromi, introduce new discover of the category.

The effects of zonisamide on L-DOPA-induced dyskinesia in Parkinson’s disease model mice

Parkinson’s disease (PD) is a neurodegenerative disorder caused by the loss of dopaminergic neurons in the midbrain and shows motor dysfunctions. Zonisamide (ZNS, 1,2-benzisoxazole-3-methanesulfonamide), which was originally developed as an antiepileptic drug, was also found to have beneficial effects on motor symptoms in PD. In the current study, we have investigated the behavioral and physiological effects of ZNS on L-DOPA-induced dyskinesia (LID) in PD model mice. Chronic administration of L-DOPA plus ZNS in PD model mice was shown to increase the duration and severity of LID compared with PD model mice that were treated with L-DOPA alone. To elucidate the neural mechanism of the effects of ZNS on LID, we examined neuronal activity in the output nuclei of the basal ganglia, i.e., the substantia nigra pars reticulata (SNr). Chronic administration of L-DOPA plus ZNS in PD mice decreased the firing rate in the SNr while they showed apparent LID. In addition, chronic treatment of L-DOPA plus ZNS in PD mice changed cortically evoked responses in the SNr during LID. In the control state, motor cortical stimulation induces the triphasic response composed of early excitation, inhibition, and late excitation. In contrast, L-DOPA plus ZNS-treated PD mice showed longer inhibition and reduced late excitation. Previous studies proposed that inhibition in the SNr is derived from the direct pathway and releases movements, and that late excitation is derived from the indirect pathway and stops movements. These changes of the direct and indirect pathways possibly underlie the effects of ZNS on LID.

Electric Literature of 57-11-4, 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 57-11-4.

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

57-11-4, Name is Stearic acid, molecular formula is C18H36O2, belongs to benzisoxazole compound, is a common compound. In a patnet, author is Mahindroo, N, once mentioned the new application about 57-11-4, SDS of cas: 57-11-4.

Novel indole-based peroxisome proliferator-activated receptor agonists: Design, SAR, structural biology, and biological activities

The synthesis and structure-activity relationship studies of novel indole derivatives as peroxisome proliferator-activated receptor (PPAR) agonists are reported. Indole, a druglike scaffold, was studied as a core skeleton for the acidic head part of PPAR agonists. The structural features (acidic head, substitution on indole, and linker) were optimized first, by keeping benzisoxazole as the tail part, based on binding and functional activity at PPAR gamma protein. The variations in the tail part, by introducing various heteroaromatic ring systems, were then studied. In vitro evaluation led to identification of a novel series of indole compounds with a benzisoxazole tail as potent PPAR agonists with the lead compound 14 (BPR1H036) displaying an excellent pharmacokinetic profile in BALB/c mice and an efficacious glucose lowering activity in KKA(y) mice. Structural biology studies of 14 showed that the indole ring contributes strong hydrophobic interactions with PPAR gamma and could be an important moiety for the binding to the protein.

If you’re interested in learning more about 57-11-4. The above is the message from the blog manager. SDS of cas: 57-11-4.

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

Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter.4246-51-9, Name is 3,3′-((Oxybis(ethane-2,1-diyl))bis(oxy))bis(propan-1-amine), SMILES is NCCCOCCOCCOCCCN, belongs to benzisoxazole compound. In a document, author is Sakuma, Shogo, introduce the new discover, COA of Formula: C10H24N2O3.

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.

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 4246-51-9 is helpful to your research. COA of Formula: C10H24N2O3.

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