A new application about 3-Bromo-10H-phenothiazine

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Potassium carbonate-mediated tandem C-S and C-N coupling reaction for the synthesis of phenothiazines under transition-metal-free and ligand-free conditions

An efficient potassium carbonate-mediated tandem C-S and C-N coupling reaction between N-(2-iodophenyl)acetamides and 2-halo-benzenethiols has been developed. This protocol affords a simple and efficient approach for the construction of phenothiazine derivatives without the need for addition of transition-metal catalyst or ligand for the first time. Furthermore, the reaction can be easily performed on a large scale.

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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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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

 

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

 

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

 

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

 

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

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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

 

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

 

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

 

Discovery of 3-Bromo-10H-phenothiazine

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The Extraction of Organic Bromo-compounds

The liquid extraction of organic bromo-compounds is discussed.The effect of the bromo-substituent on the partition coefficient depends on the activity of the extractant.The influence of the positions and numbers of bromine substituents on the partition coefficiemts is surveyed.

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

 

Extracurricular laboratory:new discovery of 1-Chloro-10H-phenothiazine

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Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors

The phenothiazine system was identified as a favorable cap group for potent and selective histone deacetylase 6 (HDAC6) inhibitors. Here, we report the preparation and systematic variation of phenothiazines and their analogues containing a benzhydroxamic acid moiety as the zinc-binding group. We evaluated their ability to selectively inhibit HDAC6 by a recombinant HDAC enzyme assay, by determining the protein acetylation levels in cells by western blotting (tubulin vs histone acetylation), and by assessing their effects on various cancer cell lines. Structure-activity relationship studies revealed that incorporation of a nitrogen atom into the phenothiazine framework results in increased potency and selectivity for HDAC6 (more than 500-fold selectivity relative to the inhibition of HDAC1, HDAC4, and HDAC8), as rationalized by molecular modeling and docking studies. The binding mode was confirmed by co-crystallization of the potent azaphenothiazine inhibitor with catalytic domain 2 from Danio rerio HDAC6.

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