Archives for Chemistry Experiments of C9H8O4

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Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors

The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC50 of ?3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Pharmacological evaluation of prazosin- and doxazosin-related compounds with modified piperazine ring

New doxazosin-related compound (1-3) with a N,N’-dimethyl alkanediamine chain replacing the piperazine ring, have been synthesized and their pharmacological properties have been tested together with some prazosin analogues (4-8) bearing either a similar structural modification or a substituted piperazine moiety. In the in vitro study, on alpha1- and alpha2-adrenoceptors of rat vas deferens tissues, 1-3 displayed high alpha1-antagonist activity, 2 and 3 being equipotent to doxazosin but markedly less selective in respect to alpha2-adrenoceptors. Replacement of the piperazine ring with an alkanediamine chain resulted in a strong fall in alpha1-selectivity, owing to increased alpha2-antagonist activity, as in the prazosin-related series. In in vivo studies, the antihypertensive activity of tested compounds was investigated on spontaneously hypertensive rats (SHR) following both intragastric (IG) and intraperitoneal (OP) administration. Among the tested compounds, 7 and 8, which conserved a substituted piperazine ring, proved the most interesting drugs displaying a marked hypotensive effect. The other prazosin- and doxazosin-related compounds, in which an alkanediamine chain replaced the piperazine nucleus, showed an antihypertensive activity markedly lower than that of parent compounds, prazosin (CAS 19216-56-9) and doxazosin (CAS 74191-85-8), although a high alpha1-antagonist activity in in vitro tests was conserved. These results suggest that the piperazine ring of the prazosin- and doxazosin-related compounds, although not crucial for alpha1-antagonist activity, may play an important role in the antihypertensive effect, probably by influencing the pharmacokinetic properties of the antagonist.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthetic Route of 70918-54-6, Irreversible inhibitors are therefore the equivalent of poisons in heterogeneous catalysis.Enzyme inhibitors cause a decrease rate of an enzyme-catalyzed reaction to a specific portion of an enzyme and thus slowing a reaction . In an article, 70918-54-6, molcular formula is C9H8O4, introducing its new discovery.

Regio- and stereoselective Pd-catalyzed direct arylation of unactivated sp3 C(3)-H bonds of tetrahydrofuran and 1,4-benzodioxane systems

An auxiliary-enabled Pd-catalyzed highly regio- and stereoselective sp3 C-H activation and the direct arylation of the C3-position of oxygen heterocycles, such as tetrahydrofuran and 1,4-benzodioxane systems, are reported. An efficient stereoselective construction of cis 2,3-disubstituted tetrahydrofuran derivatives (analogues of norlignans) and cis 2,3-disubstituted 1,4-benzodioxane derivatives (analogues of neolignans) is described. The direct C(sp3)-H arylation of the C3-position of (R)- or (S)- tetrahydrofuran-2-carboxamides furnished the corresponding (2R,3R) and (2S,3S) C3-arylated THF scaffolds as major compounds with very high regio- and diastereoselectivities. The stereochemistry of the products obtained in this work were unambiguously assigned on the basis of the X-ray structure analyses of representative compounds 3b, 3e, 4p, and 7.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Archives for Chemistry Experiments of C9H8O4

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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.In a patent, 70918-54-6, name is (S)-1,4-Benzodioxane-2-carboxylic acid, introducing its new discovery. Recommanded Product: (S)-1,4-Benzodioxane-2-carboxylic acid

Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors

The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC50 of ?3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 70918-54-6, and how the biochemistry of the body works.Recommanded Product: (S)-1,4-Benzodioxane-2-carboxylic acid

Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Can You Really Do Chemisty Experiments About C9H8O4

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 70918-54-6. In my other articles, you can also check out more blogs about 70918-54-6

Synthetic Route of 70918-54-6, The main research directions are chemical synthesis, new energy materials, nano-hybrid composite materials, preparation and modification of special coatings, and research on the structure of functional materials. we perform experiments in the lab. 70918-54-6, Name is (S)-1,4-Benzodioxane-2-carboxylic acid,introducing its new discovery.

Pharmacological evaluation of prazosin- and doxazosin-related compounds with modified piperazine ring

New doxazosin-related compound (1-3) with a N,N’-dimethyl alkanediamine chain replacing the piperazine ring, have been synthesized and their pharmacological properties have been tested together with some prazosin analogues (4-8) bearing either a similar structural modification or a substituted piperazine moiety. In the in vitro study, on alpha1- and alpha2-adrenoceptors of rat vas deferens tissues, 1-3 displayed high alpha1-antagonist activity, 2 and 3 being equipotent to doxazosin but markedly less selective in respect to alpha2-adrenoceptors. Replacement of the piperazine ring with an alkanediamine chain resulted in a strong fall in alpha1-selectivity, owing to increased alpha2-antagonist activity, as in the prazosin-related series. In in vivo studies, the antihypertensive activity of tested compounds was investigated on spontaneously hypertensive rats (SHR) following both intragastric (IG) and intraperitoneal (OP) administration. Among the tested compounds, 7 and 8, which conserved a substituted piperazine ring, proved the most interesting drugs displaying a marked hypotensive effect. The other prazosin- and doxazosin-related compounds, in which an alkanediamine chain replaced the piperazine nucleus, showed an antihypertensive activity markedly lower than that of parent compounds, prazosin (CAS 19216-56-9) and doxazosin (CAS 74191-85-8), although a high alpha1-antagonist activity in in vitro tests was conserved. These results suggest that the piperazine ring of the prazosin- and doxazosin-related compounds, although not crucial for alpha1-antagonist activity, may play an important role in the antihypertensive effect, probably by influencing the pharmacokinetic properties of the antagonist.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The important role of C9H8O4

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70918-54-6, In homogeneous catalysis, catalysts are in the same phase as the reactants. Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. In a document type is Article, and a compound is mentioned, CAS :70918-54-6, Name is (S)-1,4-Benzodioxane-2-carboxylic acid, introducing its new discovery.

Silver catalysed decarboxylative alkylation and acylation of pyrimidines in aqueous media

Decarboxylative alkylation or acylation reactions of simple pyrimidines have been developed in aqueous media. Using aliphatic carboxylic acids or 2-oxocarboxylic acids and pyrimidines as substrates and silver as the catalyst, the 4-substituted alkyl or acyl pyrimidines were isolated in moderate to good yields. This journal is

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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70918-54-6, In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of reaction. CAS : 70918-54-6, Name is (S)-1,4-Benzodioxane-2-carboxylic acid. In a Article, once mentioned of 70918-54-6.

Synthesis and antibacterial activity of cinnamaldehyde acylhydrazone with a 1,4-benzodioxan fragment as a novel class of potent ss-Ketoacyl-acyl carrier protein synthase III (FabH) inhibitor

Fatty acid biosynthesis is essential for bacterial survival. ss-Ketoacyl-acyl carrier protein (ACP) synthase III (FabH), is a particularly attractive antibacterial target, since it is central to the initiation of fatty acid biosynthesis. Three series of 21 cinnamaldehyde acylhydrazone derivatives, A3-9, B3-9, and C3-9, were synthesized and evaluated for FabH-inhibitory activity. Compound B6 showed the most potent biological activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Bacillus subtilis (minimum inhibitory concentrations (MICs) values: 1.56-3.13mug/mL) and was comparable with the positive control. Docking simulation by positioning compound B6 in the FabH structure active site was performed to explore the possible binding model.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. Safety of (S)-1,4-Benzodioxane-2-carboxylic acid, 70918-54-6, name is (S)-1,4-Benzodioxane-2-carboxylic acid. In an article,Which mentioned a new discovery about 70918-54-6

Decarboxylative Cyanation of Aliphatic Carboxylic Acids via Visible-Light Flavin Photocatalysis

An operationally simple method is disclosed for the decarboxylative cyanation of aliphatic carboxylic acids at room temperature. Riboflavin tetraacetate, which is an inexpensive organic photocatalyst, promotes the oxidation of carboxylic acids upon visible-light activation. After decarboxylation, the generated radicals are trapped by TsCN, yielding the desired nitriles without any further additive, in a redox-neutral process. Importantly, this protocol can be adapted to flow conditions.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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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.In a patent, 70918-54-6, name is (S)-1,4-Benzodioxane-2-carboxylic acid, introducing its new discovery. Product Details of 70918-54-6

WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha1-adrenoreceptor subtypes and 5-HT(1A) receptors

WB 4101 (1)-related benzodioxanes were synthesized by replacing the ethylene chain separating the amine and the phenoxy units of 1 with a cyclopentanol moiety, a feature of 6,7-dihydro-5-[[(cis-2-hydroxy-trans-3- phenoxycyclopentyl)amino]methyl]-2-methylbenzo[b]thiophen-4(5H)- one that was reported to display an intriguing selectivity profile at alpha1- adrenoreceptors. This synthesis strategy led to 4 out of 16 possible stereoisomers, which were isolated in the case of (-)-3, (+)-3, (-)-4, and (+)-4 and whose absolute configuration was assigned using a chiral building block for the synthesis of (-)-3 starting from (+)-(2R)-2,3-dihydro-1,4- benzodioxine-2-carboxylic acid ((+)-9) and (1S,2S,5S)-2-amino-5- phenoxycyclopentan-1-ol ((+)-10). The aim of this project was to further investigate whether it is possible to differentiate between these compounds with respect to their affinity for alpha1-adrenoreceptor subtypes and the affinity for 5-HT(1A) receptors, as 1 binds with high affinity at both receptor systems. The biological profiles of reported compounds at alpha1- adrenoreceptor subtypes were assessed by functional experiments in isolated rat vas deferens (alpha(1A)), spleen (alpha(1B)), and aorta (alpha(1D)) and by binding assays in CHO and HeLa cells membranes expressing the human cloned alpha1- adrenoreceptor subtypes and 5-HT(1A) receptors, respectively. Furthermore, the functional activity of (-)-3, (+)-3, (-)-4, and (+)-4 toward 5-HT(1A) receptors was evaluated by determining the induced stimulation of [35S]- GTPgammaS binding in cell membranes from HeLa cells transfected with human cloned 5-HT(1A) receptors. The configuration of the cyclopentane unit determined the affinity profile: a 1R configuration, as in (+)-3 and (-)-4, conferred higher affinity at alpha1-adrenoreceptors, whereas a 1S configuration, as in (-)-3 and (+)-4, produced higher affinity for 5-HT(1A) receptors. For the enantiomers (+)-4 and (-)-4 also a remarkable selectivity was achieved. Functionally, the stereoisomers displayed a similar alpha1- selectivity profile, that is alpha(1D) > alpha(1B) > alpha(1A), which is different from that exhibited by the reference compound 1. The epimers (-)-3 and (+)-4 proved to be agonists at the 5-HT(1A) receptors, with a potency comparable to that of 5-hydroxytryptamine.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Photocatalytic decarboxylative alkenylation of alpha-amino and alpha-hydroxy acid-derived redox active esters by NaI/PPh3 catalysis

Herein, we report the photocatalytic decarboxylative alkenylation reactions of N-(acyloxy)phthalimide derived from alpha-amino and alpha-hydroxy acids with 1,1-diarylethene, and with cinnamic acid derivatives through double decarboxylation, using sodium iodide and triphenylphosphine as redox catalysts. The reaction proceeds under mild irradiation conditions with visible blue light (440 nm or 456 nm) in an acetone solvent without recourse to transition-metal or organic dye based photoredox catalysts. The reaction proceeds via photoactivation of a transiently self-assembled chromophore from N-(acyloxy)phthalimide and NaI/PPh3. Solvation plays a crucial role in the reactivity.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem