Final Thoughts on Chemistry for 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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A one-pot, two-step synthesis of bis-pyrrolidinone tetrazoles has been established via the Ugi-Azide reaction using methyl levulinate, primary amines, isocyanides and azidotrimethylsilane with subsequent acid treatment to catalyze the lactam formation. The efficiency of the protocol was established followed by a successful transition to library production in four 24-well plates.

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

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A series of benzoxazole/benzothiazole-2,3-dihydrobenzo[b][1,4]dioxine derivatives (5a-5d and 8a-8j) was synthesized. Compounds were evaluated for binding affinities at the 5-HT1A and 5-HT2A receptors. Antidepressant activities of the compounds were screened using the forced swimming test (FST) and the tail suspension test (TST). The results indicated that the compounds exhibited high affinities for the 5-HT1A and 5-HT2A receptors and showed a marked antidepressant-like activity. Compound 8g exhibited high affinities for the 5-HT1A (Ki = 17 nM) and 5-HT2A (Ki = 0.71 nM) receptors; it also produced a decrease of the immobility time and exhibited potent antidepressant-like effects in the FST and TST in mice.

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

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Reference of 214894-89-0, Chemical Research Letters, May 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine,introducing its new discovery.

Spirocyclic amide derivatives of formula I wherein ArCH2CH2NH? represents a ²-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.

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

You Should Know Something about C10H10O3

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Research speed reading in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic. Formula: C10H10O3, In a article, mentioned the application of 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, molecular formula is C10H10O3

A series of N-(4-substituted-thiazolyl)oxamic acid derivatives were synthesized and tested for antiallergy activity in the rat PCA model.These compounds were conveniently prepared by treatment of the appropriate acetophenone with thiourea and iodine or by reaction of the chloroacetylbenzene with thiourea to give the corresponding aminothiazoles; subsequent condensation with ethyloxalyl chloride gave the thiazolyloxamates.Many of the analogues showed a 50percent inhibition at <2 mg/kg po or <0.4 mg/kg iv and were significantly more potent than disodium cromoglycate, which in the rat PCA mode l is orally inactive and gives a 50percent inhibition at 1.2 mg/kg iv.Hydrolysis of the oxamates generally resulted in enhanced activities, while substitution of the phenyl ring with a variety of substituents (e.g.,4-F, 4-OEt, and 4-NHCOCH3) did not significantly enhance the activity of the unsubstituted phenyl derivative.One of the ethanolamine salts, N-<4-(1,4-benzodioxan-6-yl)-2-thiazolyl>oxamic acid ethanolamine salt (61, PRH-836-EA), has been selected for further pharmacological evaluation.

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

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The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

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

Discover the magic of the C8H9NO2

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A useful and rapid access to libraries of N-arylbenzo[b]furo[3,2-d] pyrimidin-4-amines (1) and their novel benzo[b]thieno[3,2-d]pyrimidin-4-amine analogues (2) was investigated for the first time. Title compounds were obtained via microwave-accelerated condensation and Dimroth rearrangement of suitable anilines with N?-(2-cyanaryl)-N,N-dimethylformimidamides obtained by reaction of benzo[b]furane and benzo[b]thiophene precursors with N,N-dimethylformamide dimethyl acetal. This work also demonstrates that well-controlled parameters offer comfortable use of microwave technology and are both safe and beneficial to the environment. Some products obtained in this article exhibit interesting in vitro antiproliferative effects. Copyright

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

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Chemical Research Letters, May 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. Which mentioned a new discovery about Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

We present a convenient synthesis of novel heteroaryl-fused 3-oxo-1,4-thiazepine-5-carboxamides and 5-oxo-1,4-thiazepine-3-carboxamides using a modification of four-component Ugi condensation. We demonstrate the usefulness and versatility of the developed approach for the synthesis of variously substituted compounds and discuss the scope and limitations of the chemistry involved.

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

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Molecular docking is widely used to predict novel lead compounds for drug discovery. Success depends on the quality of the docking scoring function, among other factors. An imperfect scoring function can mislead by predicting incorrect ligand geometries or by selecting nonbinding molecules over true ligands. These false-positive hits may be considered “decoys”. Although these decoys are frustrating, they potentially provide important tests for a docking algorithm; the more subtle the decoy, the more rigorous the test. Indeed, decoy databases have been used to improve protein structure prediction algorithms and protein-protein docking algorithms. Here, we describe 20 geometric decoys in five enzymes and 166 “hit list” decoys-i.e., molecules predicted to bind by our docking program that were tested and found not to do so-for beta-lactamase and two cavity sites in lysozyme. Especially in the cavity sites, which are very simple, these decoys highlight particular weaknesses in our scoring function. We also consider the performance of five other widely used docking scoring functions against our geometric and hit list decoys. Intriguingly, whereas many of these other scoring functions performed better on the geometric decoys, they typically performed worse on the hit list decoys, often highly ranking molecules that seemed to poorly complement the model sites. Several of these “hits” from the other scoring functions were tested experimentally and found, in fact, to be decoys. Collectively, these decoys provide a tool for the development and improvement of molecular docking scoring functions. Such improvements may, in turn, be rapidly tested experimentally against these and related experimental systems, which are well-behaved in assays and for structure determination.

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

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Research speed reading in 2021.The prevalence of solvent effects has motivated developing quantitative kinetic, spectroscopic, and theoretical assessments of solvent structures and their interactions with reaction intermediates and transition states. Application In Synthesis 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

Toxoplasma gondii (T. gondii) is an apicomplexan parasite that can cause eye disease, brain disease, and death, especially in congenitally infected and immune-compromised people. Novel medicines effective against both active and latent forms of the parasite are greatly needed. The current study focused on the discovery of such medicines by exploring a family of potential inhibitors whose antiapicomplexan activity has not been previously reported. Initial screening efforts revealed that niclosamide, a drug approved for anthelmintic use, possessed promising activity in vitro against T. gondii. This observation inspired the evaluation of the activity of a series of salicylanilides and derivatives. Several inhibitors with activities in the nanomolar range with no appreciable in vitro toxicity to human cells were identified. An initial structure-activity relationship was explored. Four compounds were selected for evaluation in an in vivo model of infection, and two derivatives with potentially enhanced pharmacological parameters demonstrated the best activity profiles.

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

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A high throughput screening (HTS) hit, 1 (Plk1 Ki = 2.2 muM) was optimized and evaluated for the enzymatic inhibition of Plk-1 kinase. Molecular modeling suggested the importance of adding a hydrophobic aromatic amine side chain in order to improve the potency by a classic kinase H-donor-acceptor binding mode. Extensive SAR studies led to the discovery of 49 (Plk1 Ki = 5 nM; EC50 = 1.05 muM), which demonstrated moderate efficacy at 100 mpk in a MiaPaCa tumor model, with no overt toxicity.

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