Category: 98-89-5

Chemical Research Letters, May 2021. 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, SDS of cas: 98-89-5.

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.

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

New Advances in Chemical Research in 2021. Irreversible inhibitors are therefore the equivalent of poisons in heterogeneous catalysis. 98-89-5, Name is Cyclohexanecarboxylic acid, molecular formula is C7H12O2, Category: Benzisoxazole, belongs to benzisoxazole compound, is a common compound. In a patnet, author is Caccia, S, once mentioned the new application about 98-89-5.

The need to develop new antipsychotics that have fewer motor adverse effects and offer better treatment of negative symptoms has led to a new generation of drugs. Most of these drugs undergo extensive first-pass metabolism and are cleared almost exclusively by metabolism, except for amisulpride whose clearance is largely due to urinary excretion. Risperidone has metabolic routes in common with ziprasidone but shows differences in regard to other main pathways: the benzisoxazole moiety of risperidone is oxidised by cytochrome P450 (CYP) 2D6 to the active 9-hydroxyrisperidone, whereas the benzisothiazole of ziprasidone is primarily oxidised by CYP3A4, yielding sulfoxide and sulfone derivatives with low affinity for target receptors in vitro. Olanzapine, quetiapine and zotepine also have some common metabolic features. However, for the thienobenzodiazepine olanzapine a main metabolic route is direct conjugation at the benzodiazepine nucleus, whereas for the dibenzothiazepine quetiapine and the dibenzothiepine zotepine iris CYP3A4-mediated oxidation, leading to sulfoxidation, hydroxylation and dealkylation for quetiapine, but N-demethylation to the active nor-derivative for zotepine. Although the promising benzisoxazole (iloperidone) and benzisothiazole (perospirone) antipsychotics share some metabolic routes with the structurally related available drugs, they too have pharmacologically relevant compound-specific pathways. For some of the new antipsychotics we know the isoenzymes involved in their main metabolic pathways and the endogenous and exogenous factors that, by affecting enzyme activity, can potentially modify steady-state concentrations of the parent drug or its metabolite(s), but we know very little about others (e.g. amisulpride isomers, nemonapride). For yet others, information is scarce about the activity of the main metabolites and whether and how these contribute to the effect of the parent drug. Aging reduces the clearance of most antipsychotics, except amisulpride (which requires further evaluation) and ziprasidone. Liver impairment has little or no effect on the pharmacokinetics of olanzapine, quetiapine, risperidone (and 9-hydroxy-risperidone) and ziprasidone, but information is lacking for amisulpride. Renal impairment significantly reduces the clearance and prolongs the elimination half-life of amisulpride and risperidone. Again, studies are still not available for some drugs (zotepine) and have focused on the parent drug for others (olanzapine, quetiapine, ziprasidone) despite the fact that renal impairment would be expected to lower the clearance of more polar metabolites. Addressing these issues may assist clinicians in the design of safe and effective regimens for this group of drugs, and in selecting the best agent for each specific population.

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

Related Products of 98-89-5, 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. 98-89-5, Name is Cyclohexanecarboxylic acid, SMILES is O=C(C1CCCCC1)O, belongs to benzisoxazole compound. In a article, author is Abbady, Mohamed Saad, introduce new discover of the category.

Synthesis and biological activity of some new pyridines, pyrans, and indazoles containing pyrazolone moiety

Cyclocondensation reactions of 3-phenyl-1-(3-methyl-5-oxo-1-phenyl-2-pyrazolin-4-yl) prop-2-en-1-one (2) with active methylene reagents such as ethyl cyanoacetate, malononitrile, ethyl acetoacetate, and acetoacetanilide afforded pyrazolinyl pyridine derivatives (3 and 12), pyrazolinyl pyran derivative (9), and pyrazolinyl cyclohexene derivatives (10 and 11). Reaction of 11 with hydrazines and hydroxyl amine led to the formation of indazole derivatives (13 and 14), and benzisoxazole derivative 15. Also, reaction of 9 with different reagents gave pyrano[2,3-d][1,2,3]triazine (19) and pyrano[2,3-d]pyrimidine derivatives (20 and 21). The anti-inflammatory, analgesic, and antimicrobial activities of these compounds were determined. Compounds 13 and 14 showed good anti-inflammatory activity in comparison with the standard indomethacin, whereas compounds 4, 7, and 12 showed higher analgesic activity than the reference aspirin drug. In addition, compounds 7, 11, and 15 exhibited broad spectrum activities against all bacterial and fungal species tested.

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

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 98-89-5, Name is Cyclohexanecarboxylic acid, molecular formula is C7H12O2. In an article, author is Zhang, DY,once mentioned of 98-89-5, Computed Properties of C7H12O2.

Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists

Several fused bicyclic systems have been investigated to serve as the core structure of potent and selective 5-HT1F receptor agonists. Replacement of the indole nucleus in 2 with indazole and ‘inverted’ indazole provided more potent and selective 5-HT1F receptor ligands. Indoline and 1,2-benzisoxazole systems also provided potent 5-HT1F receptor agonists, and the 5-HT1A receptor selectivity of the indoline- and 1,2-benzisoxazole-based 5-HT1F receptor agonists could be improved with modification of the benzoyl moiety of the benzamides. Through these studies, we found that the inherent geometries of the templates, not the nature of hybridization of the linking atom, were important for the 5-HT1F receptor recognition. (C) 2004 Elsevier Ltd. All rights reserved.

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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

Related Products of 98-89-5, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 98-89-5, Name is Cyclohexanecarboxylic acid, SMILES is O=C(C1CCCCC1)O, belongs to benzisoxazole compound. In a article, author is Chauhan, Jay, introduce new discover of the category.

One-pot synthesis of 2,1-benzisoxazoles (anthranils) by a stannous chloride-mediated tandem reduction-heterocyclization of 2-nitroacylbenzenes under neutral conditions

Classically, 2,1-benzisoxazoles (anthranils) are prepared from 2-nitroacylbenzenes by a reductive heterocyclization reaction with Sn or SnCl2 concentrated HCl. Acid sensitive functionalities are expected to be incompatible with these conditions; milder approaches to the synthesis of 2,1-benzisoxazoles would be welcomed. We demonstrate that SnCl2 center dot 2H(2)O in a 1:1 mixture of EtOAc/MeOH is capable of mediating the tandem reduction-heterocyclization of a variety of 2-nitroacylbenzenes to their corresponding 2,1-benzisoxazoles in good to excellent yields under essentially neutral conditions. Importantly, several commonly used acid-labile protecting groups, including Boc carbamate, tert-butyl ether, and tert-butyl ester, proved orthogonal to these reaction conditions. (C) 2012 Elsevier Ltd. All rights reserved.

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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 98-89-5, Name is Cyclohexanecarboxylic acid. In a document, author is WANG, GJ, introducing its new discovery. Computed Properties of C7H12O2.

SYNTHESIS AND CATALYTIC PROPERTIES OF HYDROPHOBICALLY-MODIFIED POLY(ALKYLMETHYLDIALLYLAMMONIUM CHLORIDES)

Novel non-cross-linked and cross-linked, hydrophobically modified homo- and copolymers were synthesized by free-radical cyclo(co)polymerization of alkylmethyldiallylammonium chloride monomers in aqueous solution using ammonium persulfate as the initiator. Cross-linking was brought about by addition of a small amount of N,N’-methylenebisacrylamide. The cross-linked homo- and copolymers showed an increase of their reduced viscosity in aqueous solution upon the controlled introduction of cross-linking agent into their chemical structure. Viscosity measurements revealed that the conformational transition of polysoaps to compact coils in aqueous solution is strongly dependent upon the hydrophobic group content of the polysoaps. The formation of hydrophobic microdomains is akin to intramolecular micelle formation. Depending on the hydrophobic group content and the percentage of cross-linking, intermolecular aggregation was also revealed by viscosity measurements at higher concentrations of polysoap. The hydrophobic microdomains of the non-cross-linked and cross-linked polysoaps were characterized by hypsochromic shifts of the long-wavelength absorption band of Methyl Orange as a solvatochromic probe, non-covalently bound to the macromolecule. Catalysis of the unimolecular decarboxylation of 6-nitrobenzisoxazole-3-carboxylate by the non-cross-linked and crosslinked copolymers was investigated in aqueous solution at pH 11.3 and 30 degrees C. The cross-linked polysoaps exhibited higher catalytic activities for decarboxylation than the corresponding non-cross-linked analogues. A maximum in rate constant was found at about 0.2% (w/w) of cross-linking agent in the cross-linked polysoaps. The decarboxylation rate is strongly dependent upon the hydrophobic group content in the polysoaps.

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

Reference of 98-89-5, 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. 98-89-5, Name is Cyclohexanecarboxylic acid, SMILES is O=C(C1CCCCC1)O, belongs to benzisoxazole compound. In a article, author is KANBA, S, introduce new discover of the category.

THE 1ST OPEN STUDY OF ZONISAMIDE, A NOVEL ANTICONVULSANT, SHOWS EFFICACY IN MANIA

1 Zonisamide, an anticonvulsant developed in Japan, is structurally similar to serotonin. Zonisamide has been proven to have a pharmacological profile that is very similar to that of carbamazepine. Thus, the effect of zonisamide was examined in 24 psychiatric patients: 15 with bipolar manic state, 6 with schizoaffective manic state, and 3 schizophrenic excitement. 2 Approximately 25% of all the patients and 33% of the bipolar manic patients showed remarkable global improvement with the addition of zonisamide. Approximately 71% of all the patients and 80% of the bipolar group had more than moderate global improvement. 3 No serious adverse reactions were found and no patients required zonisamide withdrawal. One patient developed both leukocytosis and mildly abnormal liver function test. One developed leukocytosis and another reported mild sleepiness. These reactions disappeared when zonisamide was discontinued.

Reference of 98-89-5, 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.I hope my blog about 98-89-5 is helpful to your research.

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. 98-89-5, Name is Cyclohexanecarboxylic acid, formurla is C7H12O2. In a document, author is Li, Aitao, introducing its new discovery. Application In Synthesis of Cyclohexanecarboxylic acid.

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.

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

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 98-89-5, Name is Cyclohexanecarboxylic acid, SMILES is O=C(C1CCCCC1)O, belongs to Benzisoxazole compound. In a document, author is WANG, GJ, introduce the new discover, Name: Cyclohexanecarboxylic acid.

SYNTHESIS OF HYDROPHOBICALLY AND ELECTROSTATICALLY MODIFIED POLYACRYLAMIDES AND THEIR CATALYTIC EFFECTS ON THE UNIMOLECULAR DECARBOXYLATION OF 6-NITROBENZISOXAZOLE-3-CARBOXYLATE ANION

A series of hydrophobically and electrostatically modified polyacrylamides (Copol(AM-C12)) has been synthesized by radical-initiated copolymerization of acrylamide with n-dodecylmethyldiallylammonium bromide as the hydrophobe in aqueous solution using ammonium persulfate as the initiator. The formation of hydrophobic microdomains of the copolymers was revealed by large hypsochromic shifts of the long-wavelength absorption band of the solvatochromic probe Methyl Orange, noncovalently bound to the macromolecule. It was found that the microdomains formed by these copolymers in aqueous solution are more hydrophobic than those of the cationic polysoaps poly(alkylmethyldiallylammonium halides) containing the same n-dodecyl groups as the side chains as a result of the reduced electrostatic repulsions at the periphery of the microdomains. The reduced cationic character of the copolymers Copol(AM-C12) most likely also accounts for the observation that the anionic dye Methyl Orange does not; induce microdomain formation in aqueous solution. The effect of the hydrophobically and electrostatically modified polyacrylamides on the unimolecular decarboxylation of 6-nitrobenzisoxazole-3-carboxylate anion (6-NBIC) has been investigated in aqueous solutions at pH 11.3 and 30 degrees C. It is suggested that the relatively modest catalytic effects induced by Copol(AM-C12) should be ascribed to hydrogen-bond stabilization of the initial state by NH groups in the macromolecules. The decarboxylation rates of 6-NBIC at binding sites in hydrophobic microdomains increase with increasing n-dodecyl group content in the copolymers.

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 98-89-5 is helpful to your research. Name: Cyclohexanecarboxylic acid.

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