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Resistance of malaria parasites has quickly developed to almost all used antimalarial drugs. Accordingly, the discovery of new effective drugs to counter the spread of malaria parasites that are resistant to existing agents, especially acting on multi-targets, is an urgent need. The cysteine protease falcipain-2 (FP-2) and dihydrofolate reductase (DHFR) play crucial roles in the Plasmodium life cycle. In this study, a series of first-gereration small molecular dual inhibitor of FP-2 and DHFR have been designed and synthesized based on the lead compound 1, which was randomly identified by screening FP-2 inhibitors in our laboratory. Six compounds (2f-g, 2j, and 2m-o) showed improved dual inhibitory activities against FP-2 (IC50 = 2.7-13.2 muM) and DHFR (IC50 = 1.8-19.8 muM), and the inhibitory capability of compound 2o against FP-2 and DHFR were increased ?8 and ?6 times than that of compound 1, respectively. Moreover, compound 2o exhibited moderate in vivo antimalarial activity in a dose dependent fashion, its safety and survival rate were slightly better than that of positive drug. The preliminary SAR was obtained, meanwhile, molecular modeling result provided the key structural information to maintain the dual inhibitory activity, and was helpful for future dual inhibitors design.

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

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New research progress on 22013-33-8 in 2021. 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, 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

Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed herein.

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

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For the preparation of compound libraries of Michael acceptors with tunable reactivity toward nuclophilic selenocysteine residue of thioredoxin reductase, a range of 3-arylglutaconic acids were required. The existing methods at the time had limited scope or involved several steps. A hitherto undescribed protocol for direct palladium(II) acetate-catalyzed arylation of glutaconic acid dimethyl ester at position 3 has been developed with a diverse set of arenediazonium tosylates followed by hydrolysis. This generally good-yielding two-step sequence displayed a propensity to deliver E -configured coupling products while compounds mostly featured in the literature were predominantly Z -configured. The possibility for preparing a library of 4-arylpyridine-2,6(1 H,3 H)-diones has been exemplified.

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

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Reference of 22013-33-8,New Advances in Chemical Research in 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine,introducing its new discovery.

Pseudomonas aeruginosa is a notorious human pathogen associated with a range of life-threatening nosocomial infections. There is an increasing problem of antibiotic resistance in P. aeruginosa, highlighted by the emergence of multi-drug resistant strains. Thus the exploration of new strategies for the treatment of P. aeruginosa infections is clearly warranted. P. aeruginosa is known to produce a range of virulence factors that enhance its ability to damage the host tissue and cause disease. One of the most important virulence factors is pyocyanin. P. aeruginosa regulates pyocyanin production using an intercellular communication mechanism called quorum sensing, which is mediated by small signalling molecules termed autoinducers. One native autoinducer is N-(3-oxododecanoyl)-l-homoserine lactone (OdDHL). Herein we report the synthesis of a collection of abiotic OdDHL-mimics. A number of novel compounds capable of competing with the endogenous OdDHL and consequently, inhibiting the production of pyocyanin in cultures of wild type P. aeruginosa were identified. We present evidence suggesting that compounds of this general structural type act as direct antagonists of quorum sensing in P. aeruginosa and as such may find value as molecular tools for the study and manipulation of this signalling pathway. A direct quantitative comparison of the pyocyanin suppressive activities of the most active OdDHL-mimics with some previously-reported inhibitors (based around different general structural frameworks) of quorum sensing from the literature, was also made.

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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 category: benzodioxans, category: benzodioxans

Reduction of 3-(carboxyaryl)isocoumarins with sodium borohydride proceeds with formation of corresponding 3-carboxyaryl-3,4-dihydroisocoumarins or isomeric dihydrophthalides, 3-(2-carboxybenzyl)-2-benzofuran-1(3H)-ones. Derivatives at the carboxyl group of 3-carboxyaryl-3,4-dihydroisocoumarins and 3-(2-carboxybenzyl)-2-benzofuran-1(3H)-ones have been obtained. 0009-3122/12/4710-12122012 Springer Science+Business Media, Inc.

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

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We have designed, synthesised and characterised the effects of a number of novel anthraquinone derivatives and assessed their effects on large conductance, Ca2+ activated K+ (BK) channels recorded from rabbit bladder smooth muscle cells using the excised, inside/out configuration of the patch clamp technique. These compounds are members of the GoSlo-SR family of compounds, which potently open BK channels and shift the voltage required for half maximal activation (V1/2) negatively. The efficacy of the anilinoanthraquinone derivatives was enhanced when the size of ring D was increased, since the cyclopentane and cyclohexane derivatives shifted the V 1/2, by -24 ± 6 mV and -54 ± 8 mV, respectively, whereas the cycloheptane and cyclooctane derivatives shifted the V1/2 by -61 ± 6 mV and -106 ± 6 mV. To examine if a combination of hydrophobicity and steric bulking of this region further enhanced their ability to open BK channels, we synthesised a number of naphthalene and tetrahydro-naphthalene derivatives. The tetrahydro-2-naphthalene derivative GoSlo-SR-5-69 was the most potent and efficacious of the series since it was able to shift the activation V1/2 by greater than -100 mV when applied at a concentration of 1 muM and had an EC50 of 251 nM, making it one of the most potent and efficacious BK channel openers synthesised to date.

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

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New research progress on 22013-33-8 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 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

New azanaphtoquinone compounds with aromatic moiety were synthesized and their structures were defined by Fourier transform infrared, 13C NMR, 1H NMR and mass spectra. The activities of synthesized azanaphthoquinones as antimicrobial agents against three strains of Gram-positive, four strains of Gram-negative and as well as against three strains of fungi were also investigated. Compound 3d showed eight times greater antibacterial activity against the most sensitive organism being S. epidermidis with a MIC value of 1.22 mug/mL than the reference antimicrobial compound Cefuroxime (MIC = 9.8 mug/mL). For compound 3c, the antibacterial activity against S. epidermidis and S. aureus was equal to that of Cefuroxime and Cefuroxime-Na, respectively. The antibacterial activity of the compounds 3c and 3d were two times stronger against E. faecalis than the reference antimicrobial compound Amikacin. The results obtained in this study revealed that newly synthesized compounds 3c, 3d, and 3e are effective in treating infectious caused by especially Gram-positive bacteria have developed multiple resistances to antibiotics and are favorable structures in designing novel antimicrobial agents.

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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. Quality Control 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

The development of original strategies for the preparation of indole derivatives is a major goal in drug design. Herein, we report the first straight access to indoles from anilines and ethylene glycol by heterogeneous catalysis, based on an acceptorless dehydrogenative condensation, under noninert conditions. In order to achieve high selectivity, a combination of Pt/Al2O3 and ZnO have been found to slowly dehydrogenate ethylene glycol generating, after condensation with the amine and tautomeric equilibrium, the corresponding pyrrole-ring unsubstituted indoles.

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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. COA of Formula: C8H9NO2, 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

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

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I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 22013-33-8, help many people in the next few years.Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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