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Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu4

Using a functional high-throughput screening (HTS) and subsequent solution-phase parallel synthesis approach, we have discovered a novel series of positive allosteric modulators formGlu4, a G-protein coupled receptor. This series is comprised of a homopiperazine central core. The solution-phase parallel synthesis and SAR of analogs derived from this series will be presented. This series of positive allosteric modulators of mGlu4 provide critical research tools to further probe the mGlu4-mediated effects in Parkinson’s disease.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Column chromatography-free solution-phase synthesis of a natural piper-amide-like compound library

We have achieved an efficient solution-phase parallel synthesis of a library of natural piper-amide-like compounds from the bifunctional beta-phosphono-N-hydroxy-succinimidyl ester intermediate. The primary important feature in our study is the construction of natural-product-like molecules through the adaptation of sophisticated organic reactions that create water-soluble byproducts for a chromatography-free purification. This simple and efficient method rapidly provides a combinatorial library of high yield and purity. The library was evaluated against GPCR targets to demonstrate its potential use as a tool for drug discovery and in chemical biology.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Related Products of 22013-33-8, 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. 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2. In a Article£¬once mentioned of 22013-33-8

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£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The important role of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS

The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer?s disease, parkinson?s disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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An abnormal N-heterocyclic carbene based nickel complex for catalytic reduction of nitroarenes

Herein we report the synthesis of a nickel(ii) dichloro complex bearing an abnormal N-heterocyclic carbene (aNHC). The NiCl2(aNHC)2 complex has been used as an efficient catalyst for the reduction of nitroarenes with hydrosilanes to give aromatic amines in good to excellent yields. This catalytic protocol can tolerate functional groups such as halides, alkenes or nitriles. Furthermore, the longevity of the catalyst was tested in successive catalytic cycles, which indicates a sustained catalytic activity over multiple catalytic cycles.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Awesome and Easy Science Experiments about 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Related Products of 22013-33-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2. In a article£¬once mentioned of 22013-33-8

Discovery of novel Syk/PDGFR-alpha/c-Kit inhibitors as multi-targeting drugs to treat rheumatoid arthritis

Due to the complex biological pathways involved in rheumatoid arthritis, discovery of multi-targeting small molecules provides an effective strategy to achieve better efficacy and lower toxicity. Herein the first Syk/PDGFR-alpha/c-Kit inhibitors were designed and evaluated. Dihydrofuropyrimidine derivative 13 showed potent inhibitory activity against the three targets. Importantly, compound 13 exhibited good cellular efficacy against fibroblast-like synoviocytes (IC50 = 3.21 muM) and mouse bone marrow-derived mast cells (IC50 = 2.03 muM) and significantly decreased the secretion of inflammatory cytokines. Thus, Syk/PDGFR-alpha/c-Kit triple inhibitor 13 represented a promising lead compound for the treatment of RA.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Brief introduction of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, belongs to benzodioxans compound, is a common compound. Computed Properties of C8H9NO2In an article, once mentioned the new application about 22013-33-8.

Structure-activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl)propyl thiourea template

In an effort to design inhibitors of human glutaminyl cyclase (QC), we have synthesized a library of N-aryl N-(5-methyl-1H-imidazol-1-yl)propyl thioureas and investigated the contribution of the aryl region of these compounds to their structure-activity relationships as cyclase inhibitors. Our design was guided by the proposed binding mode of the preferred substrate for the cyclase. In this series, compound 52 was identified as the most potent QC inhibitor with an IC50 value of 58 nM, which was two-fold more potent than the previously reported lead 2. Compound 52 is a most promising candidate for future evaluation to monitor its ability to reduce the formation of pGlu-Abeta and Abeta plaques in cells and transgenic animals.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Discovery of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 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

Continuous flow hydrogenation of nitroarenes, azides and alkenes using maghemite-Pd nanocomposites

Maghemite-supported ultra-fine Pd (1-3 nm) nanoparticles, prepared by a simple co-precipitation method, find application in the catalytic continuous flow hydrogenation of nitroarenes, azides, and alkenes wherein they play an important role in the reduction of various functional groups on the surface of maghemite with catalyst loading (~6 wt% Pd). The salient features of the protocol include expeditious formation of reduced products in high yields under near ambient conditions with recycling of the catalyst (up to 12 cycles) without any decrease in selectivity and yield.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

More research is needed about 22013-33-8

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 22013-33-8 is helpful to your research. Synthetic Route of 22013-33-8

Synthetic Route of 22013-33-8, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 22013-33-8, molcular formula is C8H9NO2, introducing its new discovery.

Synthesis of 4-azo-butenolides

An efficient, catalyst-free, microwave-assisted approach has been developed for the synthesis of 4-azo-butyenolides derivatives by condensing tetronic acid with various anilines. This approach exhibited good functional group compatibility and produced the desired products in good to excellent yields in just 30?40 min. This approach can be seen as a better alternative to protocols with long reaction times used for the synthesis of these compounds, which are synthons for the obtaining of quinolines.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Thiopyrimidine and isothiazolopyrimidine kinase inhibitors

Compounds having the formula 1are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem