Month: April 2021

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

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

Electric Literature of 636-61-3, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 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 Li, Aitao, introduce new discover of the category.

A redox-mediated Kemp eliminase

The acid/base-catalysed Kemp elimination of 5-nitro-benzisoxazole forming 2-cyano-4-nitrophenol has long served as a design platform of enzymes with non-natural reactions, providing new mechanistic insights in protein science. Here we describe an alternative concept based on redox catalysis by P450-BM3, leading to the same Kemp product via a fundamentally different mechanism. QM/MM computations show that it involves coordination of the substrate’s N-atom to haem-Fe(II) with electron transfer and concomitant N-O heterolysis liberating an intermediate having a nitrogen radical moiety Fe(III)-N-center dot and a phenoxyl anion. Product formation occurs by bond rotation and H-transfer. Two rationally chosen point mutations cause a notable increase in activity. The results shed light on the prevailing mechanistic uncertainties in human P450-catalysed metabolism of the immunomodulatory drug leflunomide, which likewise undergoes redox-mediated Kemp elimination by P450-BM3. Other isoxazole-based pharmaceuticals are probably also metabolized by a redox mechanism. Our work provides a basis for designing future artificial enzymes.

Electric Literature of 636-61-3, 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 636-61-3.

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

In an article, author is Schousboe, Arne, once mentioned the application of 98-89-5, Name is Cyclohexanecarboxylic acid, molecular formula is C7H12O2, molecular weight is 128.169, MDL number is MFCD00001461, category is benzisoxazole. Now introduce a scientific discovery about this category, Category: Benzisoxazole.

Delineation of the Role of Astroglial GABA Transporters in Seizure Control

Studies of GABA transport in neurons and astrocytes have provided evidence that termination of GABA as neurotransmitter is brought about primarily by active transport into the presynaptic, GABAergic nerve endings. There is, however, a considerable transport capacity in the astrocytes surrounding the synaptic terminals, a transport which may limit the availability of transmitter GABA leading to a higher probability of seizure activity governed by the balance of excitatory and inhibitory neurotransmission. Based on this it was hypothesized that selective inhibition of astrocytic GABA transport might prevent such seizure activity. A series of GABA analogs of restricted conformation were synthesized and in a number of collaborative investigations between Prof. Steve White at the University of Utah and medicinal chemists and pharmacologists at the School of Pharmacy and the University of Copenhagen, Denmark, GABA analogs with exactly this pharmacological property were identified. The most important analogs identified were N-methyl-exo-THPO (N-methyl-3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole) and its lipophilic analog EF-1502 ((RS)-4-[N-[1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl]-N-methylamino]-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol) both of which turned out to be potent anticonvulsants in animal models of epilepsy.

Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 98-89-5, Category: Benzisoxazole.

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

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , Safety of 3-Hydroxybenzoic acid, 99-06-9, Name is 3-Hydroxybenzoic acid, molecular formula is C7H6O3, belongs to benzisoxazole compound. In a document, author is Kitamura, S, introduce the new discover.

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.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 99-06-9. Safety of 3-Hydroxybenzoic acid.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 3878-55-5, Name is 4-Methoxy-4-oxobutanoic acid, formurla is C5H8O4. In a document, author is Chandra, Sharath S. P., introducing its new discovery. COA of Formula: C5H8O4.

EFFECT OF NOVEL BENZISOXAZOLE DERIVATIVES AGAINST EHRLICH ASCITES CARCINOMA CELLS IN SWISS ALBINO MICE: CYTOTOXIC AND HAEMATALOGICAL STUDIES

The present study is to investigate the cytotoxicity properties and haematological indices of synthesized molecules (S1-S4) in comparison to the standard drug 5 fluorouracil which reflects the anticancer potentials of the above molecules. Cytotoxicity studies were performed by in vitro MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl teterazolium bromide) assay. Haematological studies were done by drawing blood in the drug and synthesized molecules administered animals by retroorbital method. Haemoglobin, RBC, WBC, lymphocytes, Monocytes and Granulocytes counts were measured. All the above experiments were performed against Ehrlich ascites carcinoma (EAC) in Swiss albino mice. The percentage cytotoxicity and percentage viable cell counts revealed anticancer properties of the synthesized molecules. RBC count indicated protection of cell membrane from destruction and the WBC counts along with lymphocytes, Monocytes and granulocytes also show the immunoprotective characteristics of the novel molecules. Thus it has been concluded that the synthesized molecules (S1-S4) if supported by further molecular studies may have a promising role to play as anticancer agents.

If you are hungry for even more, make sure to check my other article about 3878-55-5, COA of Formula: C5H8O4.

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

Synthetic Route of 815-17-8, 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. 815-17-8, Name is 3,3-Dimethyl-2-oxobutanoic acid, SMILES is CC(C)(C)C(C(O)=O)=O, belongs to benzisoxazole compound. In a article, author is Kociolek, Martin G., introduce new discover of the category.

SYNTHESIS OF 1,2-BENZISOXAZOLE 2-OXIDES

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.

Synthetic Route of 815-17-8, 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 815-17-8 is helpful to your research.

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

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 627-03-2, Name is 2-Ethoxyacetic acid, molecular formula is C4H8O3. In an article, author is Yoshimi, K,once mentioned of 627-03-2, Application In Synthesis of 2-Ethoxyacetic acid.

Novel monoamine oxidase inhibitors, 3-(2-aminoethoxy)-1,2-benzisoxazole derivatives, and their differential reversibility

Although possible usefulness of non-selective monoamine oxidase (MAO) inhibitors for Parkinson’s disease therapy has been suggested in the literature, MAO inhibitors whose inhibition is reversible and have dual action to both MAO-A and -B subtypes is not available yet. Subtype selectivity and reversibility of a series of novel MAO inhibitors, 3-(2-aminoethoxy)-1,2-benzisoxazole derivatives, were studied. Several dual MAO inhibitors, which inhibit both MAO-A and -B, were obtained. When administered to mice, their effects were generally reversible. Among the derivatives, RS-1636 and RS-1653 had much longer duration of brain MAO-B inhibition than that of MAO-A. In vitro, the inhibited MAO-A activity by these compounds was partially recovered by buffer change at 4degreesC, while little MAO-B activity was recovered. Although it is not fully elucidated yet, the reversibility of these inhibitors is probably determined primarily by this dissociation profile. This unique differential reversibility indicates that optimization of the balance of actions can be achieved by differentiating reversibility to each target molecule.

If you are hungry for even more, make sure to check my other article about 627-03-2, Application In Synthesis of 2-Ethoxyacetic acid.

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

Chemistry, like all the natural sciences, Product Details of 99189-60-3, begins with the direct observation of nature— in this case, of matter.99189-60-3, Name is 2-[1-(2-Amino-2-oxoethyl)cyclohexyl]acetic Acid, SMILES is O=C(O)CC1(CC(N)=O)CCCCC1, belongs to benzisoxazole compound. In a document, author is Byrappa, Sathish, introduce the new discover.

Synthesis and Screening of Pro-apoptotic and Angio-inhibitory Activity of Novel Benzisoxazole Derivatives both In Vitro and In Vivo

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.

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 99189-60-3. Product Details of 99189-60-3.

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