Brief introduction of 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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Electric Literature of 3080-99-7, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. Electric Literature of 3080-99-7, Name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine, molecular formula is C8H9NS. In a Article, authors is Mylari, Banavara L.£¬once mentioned of Electric Literature of 3080-99-7

1,2-Dihydro-1-oxopyrrolo<3,2,1-kl>phenothiazine-2-carboxamides and Congeners, Dual Cyclooxygenase/5-Lipoxygenase Inhibitors with Antiinflammatory Activity

A series of 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenothiazine, 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenoxazine, and 1,2-dihydro-1-oxopyrrolo<3,2,1-de>acridine-2-carboxamides were prepared by reaction of 1,2-dihydro-1-oxopyrrolo<3,2,1-kl>phenothiazine or other corresponding phenoxazine and acridan ethyl or methyl esters with appropriate amines.Several members of this family were found to be potent, dual inhibitors of cyclooxygenase and 5-lipoxygenase pathways of arachidonic acid metabolism and to have in vivo antiinflammatory activity in the rat foot edema assay.Structure-activity relationships within this family of compounds are described. 1,2-Dihydro-N-(2-thiazolyl)-1-oxopyrrolo<3,2,1-kl>phenothiazine-1-carboxamide (34) was found to be one of the best compounds to display potent cyclooxygenase/5-lipoxygenase inhibition of arachidonic acid metabolism.Its IC50s against the enzymes sourced from rat basophillic leukemia-1 (RBL-1) cells were 0.07 and 1.4 muM, respectively.It was active in the rat foot edema test for antiinflammatory effect (48percent inhibition at 33 mg/kg po) and in the mouse phenylbenzoquinone induced writhing test for analgesic effect (93percent inhibition at 32 mg/kg po).

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Simple exploration of 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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Application of 3080-99-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Gong, Hua and a compound is mentioned, Application of 3080-99-7, 3,4-Dihydro-2H-benzo[b][1,4]thiazine, introducing its new discovery.

Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORgamma/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity

We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORgammat inverse agonists. However, a majority of these compounds showed potent activity against pregnane X receptor (PXR) and modest activity against liver X receptor alpha (LXRalpha). Structure-based drug design (SBDD) led to the identification of benzothiazine and tetrahydroquinoline sulfonamide analogs which completely dialed out LXRalpha activity and were less potent at PXR. Pharmacodynamic (PD) data for compound 35 in an IL-23 induced IL-17 mouse model is discussed along with the implications of a high Ymax in the PXR assay for long term preclinical pharmacokinetic (PK) studies.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

More research is needed about 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid

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TRICYCLIC ANTIBIOTICS

Compound of formula (I): wherein A1 represents -O-, -S- or -N-R3; A2 represents -CH2-, -O-, -N-R4, -C(=O)- or -CH(O-R4)-; A3 represents C3-C8cycloalkylene; saturated and unsaturated 4 to 8-membered heterocyclodiyl with 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, which group A3 is unsubstituted or substituted; A4 represents C1-C4alkylene, C2-C4alkenylene, >C=O or a group selected from – C2H4NH-, -C2H4O-, and -C2H4S- being linked to the adjacent NR5-group via the carbon atom; and G represents aryl or heteroaryl, which is unsubstituted or substituted and R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, mercapto, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, C1-C6alkylthio, C1-C6alkylcarbonyloxy, C1-C6alkylsulfonyloxy, C1-C6heteroalkylcarbonyloxy, C5-C6heterocyclylcarbonyloxy, C1-C6heteroalkoxy, wherein heteroalkyl, heteroalkoxy groups or heterocyclyl comprise 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulphur, in which substituents the alkyl moieties are unsubstituted or further substituted; R3, R4 and R5 independently of one another, represent hydrogen or C1-C6alkyl; X1 and X2 independently of one another, represent a nitrogen atom or CR2, with the proviso that at least one of Xl and X2 represents a nitrogen atom; m is 1; and the (CH2)m moiety is optionally substituted by C1-C4alkyl; halogen, carboxy, hydroxy, C1-C4alkoxy, C1-C4-alkylcarbonyloxy, amino, mono- or di-(C1-C4alkyl)amino or acylamino n is 0, 1 or 2 or pharmaceutically acceptable salt thereof are valuable for use as a medicament for the treatment of bacterial infections.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Archives for Chemistry Experiments of 2-Cyano-phenothiazine

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Why Have Clinical Trials of Antioxidants to Prevent Neurodegeneration Failed? – A Cellular Investigation of Novel Phenothiazine-Type Antioxidants Reveals Competing Objectives for Pharmaceutical Neuroprotection

Purpose: Only a fraction of the currently established low-molecular weight antioxidants exhibit cytoprotective activity in living cells, which is considered a prerequisite for their potential clinical usefulness in Parkinson?s disease or stroke. Post hoc structure-activity relationship analyses have predicted that increased lipophilicity and enhanced radical stabilization could contribute to such cytoprotective activity. Methods: We have synthesized a series of novel phenothiazine-type antioxidants exhibiting systematic variation in their lipophilicity and radical stabilization. Phenothiazine was chosen as lead structure for its superior activity at baseline. The novel compounds were evaluated for their neuroprotective potency in cell culture, and for their primary molecular targets. Results: Lipophilicity was associated with enhanced cytoprotective activity, but only to a certain threshold (logP ? 7). Benzannulation likewise produced improved cytoprotectants that exhibited very low EC50 values of ~8?nM in cultivated neuronal cells. Inhibition of global protein oxidation was the best molecular predictor of cytoprotective activity, followed by the inhibition of membrane protein autolysis. In contrast, the inhibition of lipid peroxidation in isolated brain lipids and the suppression of intracellular oxidant accumulation were poor predictors of cytoprotective activity, primarily as they misjudged the cellular advantage of high lipophilicity. Conclusions: Lipophilicity, radical stabilization and molecular weight appear to form an uneasy triangle, in which a slightly faulty selection may readily abolish neuroprotective activity.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

A new application about 2-(Methylsulfonyl)-10H-phenothiazine

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Reference of 23503-68-6, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. Reference of 23503-68-6, Name is 2-(Methylsulfonyl)-10H-phenothiazine, molecular formula is C13H11NO2S2. In a Article, authors is Navarro, Lorena£¬once mentioned of Reference of 23503-68-6

Synthesis and biological properties of aryl methyl sulfones

A novel group of aryl methyl sulfones based on nonsteroidal anti-inflammatory compounds exhibiting a methyl sulfone instead of the acetic or propionic acid group was designed, synthesized and evaluated in vitro for inhibition against the human cyclooxygenase of COX-1 and COX-2 isoenzymes and in vivo for anti-inflammatory activity using the carrageenan induced rat paw edema model in rats. Also, in vitro chemosensitivity and in vivo analgesic and intestinal side effects were determined for defining the therapeutic and safety profile. Molecular modeling assisted the design of compounds and the interpretation of the experimental results. Biological assay results showed that methyl sulfone compounds 2 and 7 were the most potent COX inhibitors of this series and best than the corresponding carboxylic acids (methyl sulfone 2: IC50 COX-1 = 0.04 and COX-2 = 0.10 muM, and naproxen: IC50 COX-1 = 11.3 and COX-2 = 3.36 muM). Interestingly, the inhibitory activity of compound 2 represents a significant improvement compared to that of the parent carboxylic compound, naproxen. Further support to the results were gained by the docking studies which suggested the ability of compound 2 and 7 to bind into COX enzyme with low binding free energies. The improvement of the activity of some sulfones compared to the carboxylic analogues would be performed through a change of the binding mode or mechanism compared to the standard binding mode displayed by ibuprofen, as disclosed by molecular modeling studies. So, this study paves the way for further attention in investigating the participation of these new compounds in the pain inhibitory mechanisms. The most promising compounds 2 and 7 possess a therapeutical profile that enables their chemical scaffolds to be utilized for development of new NSAIDs.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Can You Really Do Chemisty Experiments About 3-Bromo-10H-phenothiazine

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Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. Safety of 3-Bromo-10H-phenothiazine, C12H8BrNS. A document type is Article, introducing its new discovery., Safety of 3-Bromo-10H-phenothiazine

Selective inhibitors of monoamine oxidase. 4. SAR of tricyclic N- methylcarboxamides and congeners binding at the tricyclics’ hydrophilic binding site

Linear [6.6.6] tricyclic moieties whose center ring is made of two atoms of differing size (here primarily thioxanth-9-ones and phenoxathiins) monosubstituted meta to the sulfur by C(O)NHMe include potent and selective inhibitors of monoamine oxidase A. Similarities with effects on SAR of acylamide and of diazapentacyclic substitution on such rings, including positional variables, the requirement for monomethylation (primary and dialkylated amides are inactive and higher monoalkylated amides show little or no potency), and that sulfur is optimally in sulfone form, suggest that binding to the enzyme occurs similarly in each series. No significantly greater rise in blood pressure was found in rats given sufficient 8 to inhibit most brain and liver MAO A and then followed by oral tyramine than was found on administration of tyramine to controls. This is in contrast to a large blood pressure rise in rats pretreated with phenelzine followed by tyramine, and in accord with the belief that an inhibitor selective for MAO A which is reversibly bound to the enzyme and therefore displaced by any ingested tyramine will not lead to the ‘cheese effect’ (hypertension during treatment with MAO inhibitors usually caused by ingestion of foods containing tyramine).

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Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Can You Really Do Chemisty Experiments About 2-Cyano-phenothiazine

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Phenothiazinimides: Atom-Efficient Electrophilic Amination Reagents

Phenothiazinimides, a fairly unknown class of imines, were prepared and found to be very reactive as ultrasimple atom-efficient electrophilic amination reagents for phenols and indoles under metal-free conditions.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Some scientific research about Methyl 3-oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylate

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Bicyclic pyrazole compounds as antibacterial agents

Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

The important role of 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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Reference of 3080-99-7, 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, 3080-99-7, molcular formula is C8H9NS, introducing its new discovery.

Regioselective synthesis of heterocycles containing nitrogen neighboring an aromatic ring by reductive ring expansion using diisobutylaluminum hydride and studies on the reaction mechanism

(Chemical Equation Presented) A systematic investigation of the reductive ring-expansion reaction of cyclic ketoximes fused to aromatic ringswith diisobutylaluminum hydride (DIBALH) is described. This reaction regioselectively afforded a variety of five- to eight-membered bicyclic heterocycles or tricyclic heterocycles containing nitrogen neighboring an aromatic ring, including indoline, 1,2,3,4,5,6-hexahydrobenz[b]azocine, 3,4-dihydro-2H-benzo[b] [1,4]oxazine, 2,3,4,5-tetrahydrobenzo[b][1,4]thiazepine, 1,2,3,4,5,6- hexahydroazepino[3,2-b]-indole, 2,3,4,5-tetrahydro-1H-benzothieno[2,3-b]azepine, 2,3,4,5-tetrahydro-1H-benzothieno[3,2-b]-azepine, 5,6-dihydrophenanthridine, and 5,6,11,12-tetrahydrodibenz[b, f]azocine. The reaction mechanism leading to the rearrangement was investigated on the basis of the restricted Becke three-parameter plus Lee-Yang-Parr (B3LYP) density functional theory (DFT) with the 6-31G (d) basis set. It was found that the reaction proceeds through a three-centered transition state via a stepwise mechanism because the potential energy curve along the intrinsic reaction coordinate (IRC) had twomaxima (saddle points; TS1 and TS2) and the partial phenonium cation intermediate C. In addition to cyclic ketoximes fused to aromatic rings, the reactions of various cyclic and acyclic ketoximeswere examined to investigate preference of migrating group. It was found that themore electron-rich group migrated preferentially to give the corresponding secondary amines.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem

 

Extended knowledge of 1-Chloro-10H-phenothiazine

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1910-85-6, Name is 1-Chloro-10H-phenothiazine, belongs to thiazines compound, is a common compound. Recommanded Product: 1910-85-6In an article, once mentioned the new application about 1910-85-6.

Learning from clinical phenotypes: Low-dose biophotonics therapies in oral diseases

This narrative review on the use of biophotonics therapies for management of oral diseases is written as a tribute to Prof. Crispian Scully. His seminal contributions to the field are highlighted by the detailed, comprehensive description of clinical presentations of oral diseases. This has enabled a more thorough, fundamental understanding of many of these pathologies by research from his group as well as inspired mechanistic investigations in many groups globally. In the same vein, a major emphasis of this narrative review is to focus on the evidence from human case reports rather than in vitro or in vivo animal studies that showcases the growing and broad impact of biophotonics therapies. The similarities and differences between two distinct forms of low-dose biophotonics treatments namely photodynamic therapy and photobiomodulation therapy are discussed. As evident in this review, a majority of these reports provide promising evidence for their clinical efficacy. However, a lack of adequate technical details, precise biological rationale, and limited outcome measures limits the current utility of these treatments. Future investigations should attempt to address these shortcomings and develop better designed, rigorous, controlled studies to fully harness the tremendous potential of low-dose biophotonics therapies.

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Reference£º
Thiazine – an overview | ScienceDirect Topics,
Thiazine | C4H5NS – PubChem