Heterocyclic Building Blocks-Benzisoxazole

Electric Literature of 25383-99-7, New discoveries in chemical research and development in 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 25383-99-7, Name is Sodium 2-((2-(stearoyloxy)propanoyl)oxy)propanoate, SMILES is O=C(C(C)OC(CCCCCCCCCCCCCCCCC)=O)OC(C)C([O-])=O.[Na+], belongs to benzisoxazole compound. In a article, author is Mimaki, T, introduce new discover of the category.

Zonisamide (1,2-benzisoxazole-3-methanesulfonamide) is a new antiepileptic drug developed in Japan. This compound is insoluble in water, and it is available in tablet and powder form. In experimental animals, this compound has been found to have a strong inhibitory effect on convulsions of cortical origin because it suppresses focal spiking and the spread of secondary generalized seizures. In humans, a series of double-blind, placebo-controlled studies revealed the efficacy of zonisamide for patients with refractory partial seizures and for selected patients with infantile spasms. Its antiepileptic mechanism of action remains unclear, but it is likely to involve blockade of both sodium and T-type calcium channels. Oral bioavailability of zonisamide is excellent in healthy human volunteers. Zonisamide is slowly absorbed and has a mean t(max) of 5 to 6 hours. Almost 100% of it is absorbed; there is no difference in bioavailability between tablets and powder. Zonisamide concentrations are highest in erythrocytes and then in whole blood and plasma. It is approximately 40% to 60% bound to plasma proteins, primarily albumin. Its volume distribution is 0.9 to 1.4 L/kg. In adults, the elimination half-life is between 50 and 62 hours, and it takes as long as 2 weeks to reach steady state. The dose-serum level correlation is linear up to doses of 10 to 15 mg/kg per day, and the therapeutic range is 10 to 40 mu g/ml. However, the relationship between serum zonisamide levels, clinical response, and adverse effects appears weak. Concurrent enzyme-inducing anticonvulsants such as phenytoin, carbamazepine, or barbiturates stimulate zonisamide metabolism and decrease serum zonisamide levels at steady state. Although zonisamide has been reported to increase the serum levels of phenytoin and carbamazepine in some patients, the interactions of zonisamide with other antiepileptic drugs seem to be of minor clinical relevance. A pilot study of zonisamide suppositories revealed that it is beneficial for patients with neurologic disorders in whom antiepileptic drugs cannot be administered by mouth.

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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. 99-14-9, Name is Propane-1,2,3-tricarboxylic acid, SMILES is O=C(O)CC(CC(O)=O)C(O)=O, in an article , author is RODRIGUEZMORGADE, S, once mentioned of 99-14-9, Quality Control of Propane-1,2,3-tricarboxylic acid.

The reaction of [2,1]benzisoxazole-4,7-quinones 1 and naphth[2,3-c]isoxazole-4,9-quinone 4 with phosphines leads to phosphoranylideneaminoquinones 2 and 5, respectively, in good to excellent yields.

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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. 181289-15-6, Name is 3-(2-Amino-2-oxoethyl)-5-methylhexanoic acid, SMILES is CC(C)CC(CC(N)=O)CC(O)=O, in an article , author is Sugihara, K, once mentioned of 181289-15-6, SDS of cas: 181289-15-6.

Zonisamide (1,2-benzisoxazole-3-methanesulfonamide) an anticonvulsant agent, is primarily metabolized to 2-sulfamoylacetyl-phenol by reductive cleavage of the 1,2-benzisoxazole ring. Rabbit liver cytosol with an electron donor of aldehyde oxidase exhibited a significant zonisamide reductase activity that was sensitive to inhibition by menadione, an inhibitor of aldehyde oxidase, The result suggested that the cytosolic activity is caused by aldehyde oxidase, a cytosolic enzyme. In fact, rabbit and rat liver aldehyde oxidase had the ability to reduce zonisamide when supplemented with its electron donor, Apparent K-M and V-max values of aldehyde oxidase for zonisamide were 217 mu M and 42 nmol/10 min/mg protein in the case of the rabbit liver enzyme, and 542 mu M and 382 nmol/10 min/mg protein in the case of the rat liver enzyme, respectively. In rabbits, hamsters, mice, and guinea pigs, zonisamide reductase activity of the liver cytosols with 2-hydroxypyrimidine, an electron donor of aldehyde oxidase, was much higher than that of the liver microsomes with NADPH. In rats, zonisamide reductase activity was examined with liver microsomes and cytosols from seven strains. The 2-hydroxypyrimidine-dependent cytosolic activity exhibited marked strain differences, unlike the NADPH-dependent microsomal activity, 1,2-Benzisoxazole was also reduced to salicylaldehyde by rabbit liver cytosol and aldehyde oxidase in the presence of 2-hydroxypyrimidine, Stoichiometric studies showed that 2-sulfamoylacetylphenol was formed accompanying nearly equimolar ammonia from zonisamide.

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

Reference of 636-61-3, New discoveries in chemical research and development in 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 636-61-3, Name is (R)-2-Hydroxysuccinic acid, SMILES is O=C(O)[C@H](O)CC(O)=O, belongs to benzisoxazole compound. In a article, author is Sambasivarao, Somisetti V., introduce new discover of the category.

OPLS-AA force field parameters have been developed and validated for use in the simulation of 68 unique combinations of room temperature ionic liquids featuring 1-alkyl-3-methylimidazolium [RMIM] (R = Me, Et, Bu, Hex, Oct), N-alkylpyridinium [RPyr], and choline cations, along with Cl-, PF6-, BF4-, NO3-, AlCl4-, Al2Cl7-, TfO-, saccharinate, and acesulfamate anions. The new parameters were fit to conformational profiles from gas-phase ab initio calculations at the LMP2/cc-pVTZ(-f)//HF/6-31 G(d) theory level and compared to experimental condensed-phase structural and thermodynamic data. Monte Carlo simulations of the ionic liquids, gave relative deviations from experimental densities of ca. 1-3% at 25 degrees C for most combinations and also yielded close agreement over a temperature range of 5 to 90 degrees C. Predicted heats of vaporization compared well with available experimental data and estimates. Transferability of the new parameters to multiple alkyl side-chain lengths for [RMIM] and [RPyr] was determined to give excellent agreement with charges and torsion potentials developed specific to desired alkyl lengths in 35 separate ionic liquid simulations. As further validation of the newly developed parameters, the Kemp elimination reaction of benzisoxazole via piperidine was computed in 1-butyl-3-methylimidazolium hexafluorophosphate [BMIM][PF6] using mixed quantum and molecular mechanics (QM/MM) simulations and was found to give close agreement with the experimental free energy of activation.

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

Electric Literature of 135236-72-5, New discoveries in chemical research and development in 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 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], belongs to benzisoxazole compound. In a article, author is Barmade, Mahesh A., introduce new discover of the category.

Nitrogen containing heterocyclic rings with an oxygen atom is considered as one of the best combination in medicinal chemistry due to their diversified biological activities. Isoxazole, a five membered heterocyclic azole ring is found in naturally occuring ibetonic acid along with some of the marketed drugs such as valdecoxib, flucloxacillin, cloxacillin, dicloxacillin, and danazol. It is also significant for showing antipsychotic activity in risperidone and anticonvulsant activity in zonisamide, the marketed drugs. This review article covers research articles reported till date covering biological activity along with SAR of fused isoxazole derivatives.

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

Reference of 929-59-9, New Advances in Chemical Research, May 2021.The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 929-59-9, Name is 1,2-Bis(2-aminoethoxy)ethane, SMILES is NCCOCCOCCN, belongs to benzisoxazole compound. In a article, author is GenreGrandpierre, A, introduce new discover of the category.

Rather efficient catalysis of the decomposition of 5-nitro-benzisoxazole to the cyanophenol was observed with antibodies elicited against a cationic hapten structurally unrelated to the benzisoxazole substrate. The rate enhancement by the most active antibody is better than 10(4) and the reaction is catalyzed by a carboxylate group associated with a hydrophobic binding site. (C) 1997 Elsevier Science Ltd.

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

Related Products of 79-14-1, New Advances in Chemical Research, May 2021.Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur, causing turnover rates to depend strongly on interfacial structure and composition. 79-14-1, Name is 2-Hydroxyacetic acid, SMILES is O=C(O)CO, belongs to benzisoxazole compound. In a article, author is Mahindroo, N, introduce new discover of the category.

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.

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

Research speed reading in 2021.Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis., Recommanded Product: 4-Methoxy-4-oxobutanoic acid, Introducing a new discovery about 3878-55-5, Name is 4-Methoxy-4-oxobutanoic acid, molecular formula is C5H8O4, belongs to benzisoxazole compound. In a document, author is Yoon, Ho-Kyoung.

Objective: Delirium is a life-threatening neuropsychiatric syndrome characterised by disturbances in consciousness, attention, cognition and perception. Antipsychotics are considered the drugs of choice in managing the symptoms of delirium. Paliperidone is a benzisoxazole derivative and the principal active metabolite of risperidone. In this study, we aimed to evaluate the efficacy of paliperidone for the treatment of delirium. Methods: A prospective open-label study of paliperidone for delirium treatment was performed with 6-day follow-up. Fifteen patients who met Diagnostic and Statistical Manual of Mental disorders, Fourth Edition criteria for delirium and had a score of 13 on the Delirium Rating Scale were recruited. The starting dose was 3 mg once a day and the dose was adjusted depending on the status of delirium. Daily assessments of the severity of delirium were evaluated using Memorial Delirium Assessment Scale (MDAS). Results: The mean daily maintenance dose of paliperidone was 3.75 +/- 1.06. The MDAS scores before and after treatment (day 7) were 23.60 +/- 6.31 and 11.33 +/- 5.45 (t = 6.78, p < 0.001), respectively. The intensity of delirium showed a statistically significant reduction in MDAS scores from the first day of treatment. No serious adverse effects were observed, and none of the patients discontinued paliperidone because of adverse effects. Conclusions: This study shows that low-dose paliperidone is effective in reducing behavioural disturbances and symptoms in delirium and is well tolerated in delirious patients. This trial is an open-label study with a small sample size, and further controlled studies will be necessary. Interested yet? Keep reading other articles of 3878-55-5, you can contact me at any time and look forward to more communication. Recommanded Product: 4-Methoxy-4-oxobutanoic acid.

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

New research progress on 99189-60-3 in 2021. Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 99189-60-3, Name is 2-[1-(2-Amino-2-oxoethyl)cyclohexyl]acetic Acid, SMILES is O=C(O)CC1(CC(N)=O)CCCCC1, in an article , author is Guo, Sheng, once mentioned of 99189-60-3, COA of Formula: https://www.ambeed.com/products/99189-60-3.html.

A mild and practical method for the catalytic installation of the amino group across alkenes and alkynes has long been recognized as a significant challenge in synthetic chemistry. As the direct hydroamination of olefins using ammonia requires harsh conditions, the development of suitable electrophilic aminating reagents for formal hydroamination methods is of importance. Herein, we describe the use of 1,2-benzisoxazole as a practical electrophilic primary amine source. Using this heterocycle as a new amino group delivery agent, a mild and general protocol for the copper-hydride-catalyzed hydroamination of alkenes and alkynes to form primary amines was developed. This method provides access to a broad range of chiral alpha-branched primary amines and linear primary amines, as demonstrated by the efficient synthesis of the antiretroviral drug maraviroc and the formal synthesis of several other pharmaceutical agents.

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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. 532-32-1, Name is Sodium benzoate, SMILES is O=C([O-])C1=CC=CC=C1.[Na+], in an article , author is LEWIS, C, once mentioned of 532-32-1, Application In Synthesis of Sodium benzoate.

The catalytic antibody 21D8 efficiently catalyzes the decarboxylation of a substituted 3-carboxybenzisoxazole-a simple, unimolecular reaction that is not susceptible to general acid/base catalysis but that is highly sensitive to the microenvironment. The transition-state structure of this decarboxylation reaction has been probed by measuring the carbon kinetic isotope effect for the uncatalyzed decarboxylation in water and for the dioxane-accelerated and antibody-catalyzed reactions. The isotope effect for the decarboxylation of 5-nitro-3-carboxybenzisoxazole is k12/k13 = 1.046 in aqueous buffer at 20-degrees-C and 1.048 for the antibody-catalyzed reaction. With increasing dioxane in the reaction medium, the rate of the spontaneous decarboxylation increases by almost four orders of magnitude, whereas the isotope effect displays only a slight, progressive decrease to k12/k13 = 1.043 in 100% dioxane. Together, these results indicate that the structure of the transition state undergoes very little change in spite of > 10(4)-fold increases in the rate of the reaction caused by solvation of the substrate by organic solvents or the low dielectric environment of the antibody active site.

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