Day: May 7, 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.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

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. 10288-72-9, In a article, mentioned the application of 10288-72-9, Name is 6-Hydroxy-1,4-benzodioxane, molecular formula is C8H8O3

PROTEIN KINASE INHIBITORS FOR PROMOTING LIVER REGENERATION OR REDUCING OR PREVENTING HEPATOCYTE DEATH

The invention relates to MKK4 (mitogen-activated protein kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The MKK4 inhibitors selectively inhibit protein kinase MKK4 over protein kinases JNK and MKK7.

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

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. Safety of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, In a article, mentioned the application of 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2

Discovery and optimization of imidazo[1,2-a]pyridine inhibitors of insulin-like growth factor-1 receptor (IGF-1R)

The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an optimized compound is also highlighted.

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

In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. Recommanded Product: 22013-33-8, 22013-33-8, name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine. In an article，Which mentioned a new discovery about 22013-33-8

Modular synthesis of bis- and tris-1,2,3-triazoles by permutable sequential azide-aryne and azide-alkyne cycloadditions

A modular synthetic method for bis- and tris-1,2,3-triazoles that include a benzotriazole structure was developed on the basis of sequential azide-aryne and azide-alkyne cycloadditions. The key to success was efficient halogen-metal exchange reaction-mediated generation of aryne from ortho-iodoaryl triflates bearing a base-sensitive terminal alkyne moiety, which was achieved using trimethylsilylmethyl Grignard reagent.

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

Electric Literature of 22013-33-8, 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 :22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, introducing its new discovery.

Inhibitors for human glutaminyl cyclase by structure based design and bioisosteric replacement

The inhibition of human glutaminyl cyclase (hQC) has come into focus as a new potential approach for the treatment of Alzheimer’s disease. The hallmark of this principle is the prevention of the formation of Abeta 3,11(pE)-40,42, as these Abeta-species were shown to be of elevated neurotoxicity and likely to act as a seeding core leading to an accelerated formation of Abeta-oligomers and fibrils. Starting from 1-(3-(1H-imidazol-1- yl)propyl)-3-(3,4-dimethoxyphenyl)thiourea, bioisosteric replacements led to the development of new classes of inhibitors. The optimization of the metal-binding group was achieved by homology modeling and afforded a first insight into the probable binding mode of the inhibitors in the hQC active site. The efficacy assessment of the hQC inhibitors was performed in cell culture, directly monitoring the inhibition of Abeta3,11(pE)-40,42 formation. 2009 American Chemical Society.

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

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. name: 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, However, they have proven to be challenging because of the mutual inactivation of both catalysts. 214894-89-0, name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine. In an article，Which mentioned a new discovery about 214894-89-0

Effect of O6-substituted guanine analogs on O6-methylguanine DNA-methyltransferase Expression and glioblastoma cells viability

Background: Glioblastoma multiforme (GBM) is often associated with a poor survival prognostic for patients. The main reason seems to be the acquired or inherent resistance to the chemotherapeutic agent used to treat the tumor, temozolomide (TMZ). To this day, the most recognized pathway of resistance is the DNA Direct Repair pathway by the means of the protein O6-methylguanine DNA-methyltransferase (MGMT). Objectives: To design and synthesize a series of MGMT inhibitors that can sensitize GBM cells to TMZ. Methods: Twenty-five O6-alkyl, O6-aryl and O6-substituted-aryl guanine analogs including nine novel compounds were synthesized, characterized, analyzed by molecular docking and tested on the T98G GBM cells viability. Results: Following molecular modeling with MGMT, the newly designed compounds 19, 22, and 24 emerged as the most promising MGMT ligands and displayed modest cytotoxicity. Guanine analog (19), bearing a p-nitrobenzyl moiety, reduced considerably the O6-methylguanine DNA-methyltransferase expression level. When combined with TMZ (1), which is used as first line treatment for brain tumors, compounds 19, 22, and 24 decreased T98G cellsoproliferation by 32%, 68% and 50%, respectively. TMZ (1) displayed negligible effect on the proliferation of these cells further supporting the notion that this cell model is resistant to this alkylating agent. Conclusion: Overall, these results notably highlight a group of MGMT inhibitors that warrants further exploration in the development of therapeutic options to circumvent TMZ resistance in brain tumors.

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

Electric Literature of 4442-53-9, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption.In a document type is Patent, and a compound is mentioned, 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, introducing its new discovery.

AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS

Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the com­pounds and using the compounds for treatment of dis­eases associated with LRRK2 receptor, such as Parkin­son?s disease

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

Related Products of 261767-10-6, 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, 261767-10-6, molcular formula is C11H12O4, introducing its new discovery.

DIHYDROBENZODIOXINE CARBOXAMIDE AND KETONE DERIVATIVES

This invention relates to certain 5-HT 4 receptor modulators, particularly 5-HT 4 receptor antagonists, represented by Formula I: wherein Z is formula (A) or (B): wherein R 1, R 2, R 3, R 4, and R 5 and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.

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

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

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