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Synthesis of N-Substituted (2,3-Dihydro-1,4-Benzodioxin-6-YL)Benzenesulfonamide Derivatives as Potent Antibacterial Agents and Moderate Enzyme Inhibitors

The present research work involved the reaction of 2,3-dihydro-1,4-benzodioxin-6-amine (1) and benzenesulfonyl chloride (2) under dynamic pH control at 10 using aqueous Na2CO3. This reaction yielded 2,3-dihydro-1,4-benzodioxin-6-yl)benzenesulfonamide (3), which was further substituted at N-position with various alkyl/aryl halides (4a ? 4m) in N,N-dimethylformamide and catalytic amount of lithium hydride to obtain N-substituted (2,3-dihydro-1,4-benzodioxin-6-yl)benzenesulfonamides (5a ? 5m). The projected structures of the synthesized derivatives were confirmed using various spectral techniques (IR, 1H NMR and EIMS). The synthesized derivatives were screened for antibacterial potential and inhibitory activity against lipoxygenase enzyme.

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

Properties and Exciting Facts About 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

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Design, synthesis and evaluation of 2-aminothiazole derivatives as sphingosine kinase inhibitors

Sphingosine kinases (SphK1, SphK2) are main regulators of sphingosine-1-phosphate (S1P), which is a pleiotropic lipid mediator involved in numerous physiological and pathophysiological functions. SphKs are targets for novel anti-cancer and anti-inflammatory agents that can promote cell apoptosis and modulate autoimmune diseases. Herein, we describe the design, synthesis and evaluation of an aminothiazole class of SphK inhibitors. Potent inhibitors have been discovered through a series of modifications using the known SKI-II scaffold to define structure-activity relationships. We identified N-(4-methylthiazol-2-yl)-(2,4?-bithiazol)-2?-amine (24, ST-1803; IC50values: 7.3 muM (SphK1), 6.5 muM (SphK2)) as a promising candidate for further in vivo investigations and structural development.

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

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PURINE DERIVATIVES USEFUL AS HSP90 INHIBITORS

The present application provides substituted purine derivatives and related compounds of the formulas shown. These compounds are useful as inhibitors of HSP90, and hence in the treatment of related diseases. (Formulae) Z1-Z3 , Xa-Xc, X2 , 324, Y and R are as defined in the specification

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Related Products of 22013-33-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2. In a Patent£¬once mentioned of 22013-33-8

ANTIPSYCHOTIC PIPERIDINE DERIVATIVES

The present invention relates to therapeutically active piperidine derivatives, of formula 1 STR1 wherein, R 1, R 2, A, X and Y are as defined in the specification. The compounds are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.

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

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Reference 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.

Fragment screening of human aquaporin 1

Aquaporins (AQPs) are membrane proteins that enable water transport across cellular plasma membranes in response to osmotic gradients. Phenotypic analyses have revealed important physiological roles for AQPs, and the potential for AQP water channel modulators in various disease states has been proposed. For example, AQP1 is overexpressed in tumor microvessels, and this correlates with higher metastatic potential and aggressiveness of the malignancy. Chemical modulators would help in identifying the precise contribution of water channel activity in these disease states. These inhibitors would also be important therapeutically, e.g., in anti-cancer treatment. This perceived importance contrasts with the lack of success of high-throughput screens (HTS) to identify effective and specific inhibitors of aquaporins. In this paper, we have screened a library of 1500 ?fragments?, i.e., smaller than molecules used in HTS, against human aquaporin (hAQP1) using a thermal shift assay and surface plasmon resonance. Although these fragments may not inhibit their protein target, they bound to and stabilized hAQP1 (sub mM binding affinities (KD), with an temperature of aggregation shift DeltaTagg of +4 to +50 C) in a concentration-dependent fashion. Chemically expanded versions of these fragments should follow the determination of their binding site on the aquaporin surface.

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

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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. Quality Control of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amineIn an article, once mentioned the new application about 22013-33-8.

Antitumor agents. 123. Synthesis and human DNA topoisomerase II inhibitory activity of 2′-chloro derivatives of etoposide and 4beta-(arylamino)-4′-O- demethylpodophyllotoxins

The 2′-chloro derivatives of etoposide and 4beta-(arylamino)-4′-O- demethylpodophyllotoxins have been synthesized and evaluated for their inhibitory activity against the human DNA topoisomerase II as well as for their activity in causing cellular protein-linked DNA breakage. The results showed that none of the compounds are active as a result of the C-2′ chloro substitution on ring E. This would suggest that the free rotation of ring E is essential for the aforementioned enzyme inhibitory activity. In addition, these 2′-chloro derivatives showed no significant cytotoxicity (KB).

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Application of 22013-33-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.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

Copper-promoted sandmeyer difluoromethylthiolation of aryl and heteroaryl diazonium salts

An efficient copper-promoted difluoromethylthiolation of aryl and heteroaryl diazonium salts is described. The reaction is conducted under mild reaction conditions and various functional groups were compatible. In addition, reactions of heteroaryl diazonium salts such as pyridyl, quinolinyl, benzothiazolyl, thiophenyl, carbazolyl, and pyrazolyl diazonium salts occurred smoothly to afford the medicinally important difluoromethylthiolated heteroarenes. Furthermore, a more practical one-pot direct diazotization and difluoromethylthiolation protocol was developed, and it converts the aniline derivatives into difluoromethylthiolated arenes. The utility of the method is demonstrated by difluoromethylthiolation of a number of natural products and drug molecules. A dose of salt: The title reaction is conducted under mild reaction conditions and various functional groups are compatible. (Hetero)aryl diazonium salts reacted smoothly to afford the medicinally important difluoromethylthiolated (hetero)arenes. A practical one-pot direct diazotization and difluoromethylthiolation protocol was developed for aniline derivatives to generate difluoromethylthiolated arenes.

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

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. COA of Formula: C8H9NO2, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 22013-33-8, in my other articles.

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Strategic tuning of excited-state properties of electroluminescent materials with enhanced hot exciton mixing

Deep blue emitters with excellent stability, high quantum yield and multifunctionality are the major issues for full-color displays. In line with this, new multifunctional, thermally stable blue emitters viz., N-(4-(10-(1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1H-phenanthro[9,10-d]imidazol-2-yl)anthracen-9-yl)phenyl)-N-phenylbenzenamine (DPIAPPB) and 2-(10-(9H-carbazol-9-yl)anthracen-9-yl)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1H-phenanthro[9,10-d]imidazole (CADPPI) with hybridized local charge transfer state (HLCT) and hot exciton properties have been synthesized. These molecules show high photoluminescence quantum yield (Phis/f): (DPIAPPB-0.82/0.70 and CADPPI-0.91/0.83). The CADPPI based device (EL-467 nm) shows high efficiencies [etac-9.85 cd A-1; etap-10.84 lm W-1; etaex-4.78% at 2.8 V; CIE (0.15, 0.10)] compared to the DPIAPPB device (EL – 472 nm) [etac-6.56 cd A-1; etap-6.16 lm W-1; etaex-4.15% at 2.8 V with CIE (0.15, 0.12)]. The green device with CADPPI:Ir(ppy)3 exhibits a maximum L-59 012 cd m-2; etaex-16.8%; etac-37.3 cd A-1; etap-39.8 lm W-1 with CIE (0.30, 0.60) and the red device with CADPPI:Ir(MDQ)2(acac) shows a maximum L-43 456 cd m-2; etaex-21.9%; etac-36.0 cd A-1; etap-39.6 lm W-1 with CIE (0.64, 0.35).

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

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Discovery of imidazole carboxamides as potent and selective CCK1R agonists

High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides. Compound 44, which was profiled extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Gold-Catalyzed Post-Ugi Cascade Transformation for the Synthesis of 2-Pyridones

A gold-catalyzed post-Ugi cascade transformation for the synthesis of 2-pyridones is described. The process involves furan?alkyne cyclization followed by furan ring-opening and cleavage of the isocyanide-originated fragment. The initially formed cis double bond can isomerize into a more stable trans double bond upon prolonged exposure to a strong Br¡ãnsted acid. Thus, the overall strategy provides a viable access towards two types of 2-pyridones.

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