9/28 News Decrypt The Mystery Of C7H6O3

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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.

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

9/28 News The Best Chemistry compound: C8H10O4

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Research speed reading in 2021. Chemistry, like all the natural sciences, begins with the direct observation of nature— in this case, of matter. Recommanded Product: 3-(Methoxycarbonyl)bicyclo[1.1.1]pentane-1-carboxylic 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. 83249-10-9, Name is 3-(Methoxycarbonyl)bicyclo[1.1.1]pentane-1-carboxylic acid, molecular formula is C8H10O4. In an article, author is Haggam, Reda A.,once mentioned of 83249-10-9.

Microwave-promoted syntheses of fluoren-9-ones and benzisoxazoles

Synthesis of some new fluoren-9-ones and benzisoxazoles under both thermal and microwave conditions is reported. The prepared products under microwave conditions are obtained with high yields and within shorter reaction times. Reaction of lithiated bromobenzene with aromatic aldehydes 2a,b delivered diarylmethanols 3a,b that were oxidized to 4a,b. Compound 4a was cyclized to give methoxyfluoren-9-one 5, which was demethylated affording hydroxyfluoren-9-one 6. Compound 4b was reacted with triethyl phosphite to produce benzisoxazole 10. On the other hand, reaction of triethyl phosphite with 13a,b afforded a mixture of phosphoramidates 14a,b and benzisoxazoles 15a,b. The structures of the synthesized compounds have been elucidated unambiguously by NMR-spectroscopic methods including HH COSY, HSQC, and HMBC experiments.

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

28-Sep-21 News More research is needed about C8H14O4

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Antibacterial Spiropyrimidinetriones with N-Linked Azole Substituents on a Benzisoxazole Scaffold Targeting DNA Gyrase

Herein, we report spiropyrimidinetriones (SPTs) incorporating N-linked azole substituents on a benzisoxazole scaffold with improved Gram-positive antibacterial activity relative to previously described analogues. SPTs have an unusual spirocyclic architecture and represent a new antibacterial class of bacterial DNA gyrase and topoisomerase IV inhibitors. They are not cross-resistant to fluoroquinolones and other DNA gyrase/topoisomerase IV inhibitors used clinically. The activity of the SPTs was assessed for DNA gyrase inhibition, and the antibacterial activity across Gram-positive and Gram-negative pathogens with N-linked 1,2,4-triazoles substituted on the 5-position provides the most worthwhile profile. Directed nucleophilic and electrophilic chemistry was developed to vary this 5-position with carbon, nitrogen, or oxygen substituents and explore structure-activity relationships including those around a target binding model. Compounds with favorable pharmacokinetic parameters were identified, and two compounds demonstrated cidality in a mouse model of Staphylococcus aureus infection.

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

9/28 News The Best Chemistry compound: C5H10O2

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 75-98-9. Application In Synthesis of Pivalic acid.

While the job of a research scientist varies, most chemistry careers in research are based in laboratories, where research is conducted by teams following scientific methods and standards.75-98-9, Name is Pivalic acid, SMILES is CC(C)(C)C(O)=O, in an article , author is NUHRICH, A, once mentioned of 75-98-9, Application In Synthesis of Pivalic acid.

SYNTHESIS AND INHIBITORY EFFECTS ON PLATELET-AGGREGATION OF 3-(2-THIENYL)- AND 3-(1-IMIDAZOLYL)-1,2-BENZISOXAOLE DERIVATIVES

A series of 3-(2-thienyl)- and 3-(1-imidazolyl)-1,2-benzisoxazoles as well as some isomeric benzoxazoles were synthesized and tested in vitro for their inhibitory effect on arachidonic acid-induced human platelet aggregation. The most active compound (7-methoxy-3-(2-thienyl)-1,2-benzisoxazole 5c) was nearly 20-30-fold more potent than acetylsalicylic acid in inhibiting platelet aggregation. Structure-activity relationships within the series are briefly discussed.

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

28-Sep News Extracurricular laboratory: Discover of C9H16O4

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BENZISOXAZOLE-3-CARBOXAMIDE AND BENZISOTHIAZOLE-3-CARBOXAMIDE AS POTENTIAL ATYPICAL ANTIPSYCHOTIC AGENTS

A series of benzisoxazole- and benzisothiazole-3-carboxamides has been prepared and tested for potential antipsychotic activity. In general, the compounds showed an affinity for dopamine D-2 and serotonin 5HT(2A) and 5HT(1A) receptors. Several Members of this series have demonstrated activity in animal models predictive of potential antipsychotic activity. In addition, compounds 18, 19, 22, 27, 28, 43, and 44 have also shown a potential for reduced EPS liability as suggested by the ratio of activity seen in mesolimbic-mediated vs nigrostriatal-mediated behavioral assays.

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

28-Sep News Final Thoughts on Chemistry for C6H12O3

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Cytokinin-like activity of N ‘-substituted N-phenylureas

We have synthesized 14 N-phenylurea derivatives, differing in the heterocyclic portion linked in N’-position, and tested their cytokinin-like activity. Three different bioassays were used: the chlorophyll level determination test, the bioassay for the expression of hormone-induced chimeric Pg5-GUS gene and the tomato regeneration test, in which 1,2-benzisoxazole-3-acetic acid (BOAA) was utilized as auxin. The cytokinin-like activity showed by three of these compounds in the regeneration assay seems to be related to their different heterocyclic nature. Results obtained indicate that the N-phenyl-N’-1,3,4-thiadiazol-2-ylurea (compound 4), an isomer of N-phenyl-N’- 1,2,3-thiadiazol-5-ylurea (thidiazuron, TDZ), in the absence of auxin induces shoot regeneration in the 34,2% of the explants cultured; the N-plienyl-N’-(3-chloro-1,2-benzisothiazol-7-yl) urea (compound 10), structurally different from TDZ, in the absence of auxin induces shoot regeneration in the 25,9% of explants, significantly lower than that of TDZ (68,8%). N-phenyl-N’-benzothiazol-6-ylurea (compound 13), structurally different from TDZ, in the absence of auxin induces the 99,5% of shoot regeneration, significantly different from that of the other substances. The addition of auxin in the cotyledon regeneration assay reduces the differences. The compound 13 could be considered a new phenylurea derivative with a highly specific cytokinin-like activity.

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

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

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 526-83-0, in my other articles. Product Details of 526-83-0.

New discoveries in chemical research and development in 2021.Product Details of 526-83-0, 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. 526-83-0, Name is 2,3-Dihydroxysuccinic acid, molecular formula is C4H6O6. In an article, author is BRANCA, C,once mentioned of 526-83-0.

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

09/28/21 News A new application about C9H17NO3

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The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 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 Acosta-Silva, Carles, once mentioned of 181289-15-6, Related Products of 181289-15-6.

Kemp Elimination Reaction Catalyzed by Electric Fields

The Kemp elimination reaction is the most widely used in the de novo design of new enzymes. The effect of two different kinds of electric fields in the reactions of acetate as a base with benzisoxazole and 5-nitrobenzisoxazole as substrates have been theoretically studied. The effect of the solvent reaction field has been calculated using the SMD continuum model for several solvents; we have shown that solvents inhibit both reactions, the decrease of the reaction rate being larger as far as the dielectric constant is increased. The diminution of the reaction rate is especially remarkable between aprotic organic solvents and protic solvents as water, the electrostatic term of the hydrogen bonds being the main factor for the large inhibitory effect of water. The presence of an external electric field oriented in the direction of the charge transfer (z axis) increases it and, so, the reaction rate. In the reaction of the nitro compound, if the electric field is oriented in an orthogonal direction (x axis) the charge transfer to the NO2 group is favored and there is a subsequent increase of the reaction rate. However, this increase is smaller than the one produced by the field in the z axis. It is worthwhile mentioning that one of the main effects of external electric fields of intermediate intensity is the reorientation of the reactants. Finally, the implications of our results in the de novo design of enzymes are discussed.

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

28-Sep News Extended knowledge of C9H17NO3

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 181289-15-6 is helpful to your research. Application In Synthesis of 3-(2-Amino-2-oxoethyl)-5-methylhexanoic acid.

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BENZISOXAZOLE-3-CARBOXAMIDE AND BENZISOTHIAZOLE-3-CARBOXAMIDE AS POTENTIAL ATYPICAL ANTIPSYCHOTIC AGENTS

A series of benzisoxazole- and benzisothiazole-3-carboxamides has been prepared and tested for potential antipsychotic activity. In general, the compounds showed an affinity for dopamine D-2 and serotonin 5HT(2A) and 5HT(1A) receptors. Several Members of this series have demonstrated activity in animal models predictive of potential antipsychotic activity. In addition, compounds 18, 19, 22, 27, 28, 43, and 44 have also shown a potential for reduced EPS liability as suggested by the ratio of activity seen in mesolimbic-mediated vs nigrostriatal-mediated behavioral assays.

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 181289-15-6 is helpful to your research. Application In Synthesis of 3-(2-Amino-2-oxoethyl)-5-methylhexanoic acid.

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

28-Sep News Now Is The Time For You To Know The Truth About C9H17NO3

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Reactivity of 2,1-Benzisoxazole in Palladium-Catalyzed Direct Arylation with Aryl Bromides

The Pd-catalyzed direct arylation of 2,1-benzisoxazole with aryl bromides to access 3-arylbenzoisoxazoles proceeds in moderate-to-high yields with 1mol% Pd(OAc)(2) or 2mol% PdCl(C3H5)(dppb) (dppb=1,4-bis(diphenylphosphino)butane) as the catalysts and KOAc as an inexpensive base. A wide variety of (hetero)aryl bromides have been employed successfully. Moreover, arylations followed by benzisoxazole ring opening allowed the preparation of 2-aminobenzophenones in only two steps.

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