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Topically applied azaphenothiazines inhibit experimental psoriasis in mice

The therapeutic efficacy of topically applied azaphenothiazine derivatives: 9-chloro-6-acetylaminobutylquinobenzo[3,2-b] [1,4]thiazine (compound 4) and 6-chloroethylureidoethyldiquino[3,2-b;2′;3′-e] [1,4]thiazine (compound 5) in the amelioration of inflammatory symptoms of imiquimod-induced psoriasis in mice was investigated. Clobederm (R), containing clobetasol propioniate, served as a reference drug. The application of the compounds led to thinning of the epidermis and reduction of the cell layers. The suppressive actions of the compounds were even stronger with regard to pathological changes of the dermis. The compounds also exerted generalized, anti-inflammatory effects by decreasing the number of circulating leukocytes, lowering subiliac lymph node weight and partially normalizing an altered blood cell composition. The changes in the composition of main cell types in the epidermis and dermis were less affected by the compounds. In addition, both compounds inhibited to a similar degree production of tumor necrosis factor alpha (TNF alpha) in human whole blood cell culture. Whereas compound 5 strongly inhibited IL-8 and CXCL10 chemokines in human keratinocytes – KERTr cell line, transfected with poly(I:C), the suppressive action of compound 4 in this model was weak. In addition, compound 5, but not compound 4, exhibited at low doses proapoptotic properties with regard to colonic cell lines. In summary, we demonstrated the therapeutic potential of two selected azaphenotiazines in the amelioration of the skin pathology elicited in a mouse experimental model of psoriasis.

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

 

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Basic Ionic Liquid Promoted Domino Knoevenagel-Thia-Michael Reaction: An Efficient and Multicomponent Strategy for Synthesis of 1,3-Thiazines

An efficient, three-component strategy for synthesis of 1,3-thiazines with high atom economy in one-pot mediated by room temperature basic ionic liquid is described here. The strategy involves basic ionic liquid, [bmim]OH-catalyzed Knoevenagel condensation between ethyl cyanoacetate and aromatic aldehyde and subsequent thia-Michael addition with substituted thioureas. The reaction sequence is smooth and quantitative under ambient temperature. [bmim]OH was recovered and reused four times without any appreciable decrease in its reactivity and product yield.

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

 

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Three-Component Coupling Reactions of Maleimides, Thiols, and Amines: One-Step Construction of 3,4-Heteroatom-functionalized Maleimides by Copper-Catalyzed C(sp(2))-H Thioamination

A copper-catalyzed intermolecular thioamination of maleimides with thiols and amines has been developed. A diverse range of 3-amino-4-thiomaleimides and 3,4-dihydropyrrolo[3,4-b][1,4]thiazine-5,7(2H,6H)-diones were obtained with good yields, involving C-N and C-S bond formations. This methodology is very practical and features high atom economy, excellent functional group tolerance.

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

 

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Mortino (Vaccinium floribundum Kunth) berry assisted green synthesis and photocatalytic performance of Silver-Graphene nanocomposite

Mortitio (Vacciniumf/oribundum Kunth) is a wild shrub native to South America, whose berries are widely consumed in Ecuador as fresh fruit, juice and jam. We reported a green synthesis of Silver-Graphene (Ag-G) nanocomposite through the reduction of Ag+ and graphene oxide using berry extract of Morthio. Silver nanoparticles were anchored onto the graphene sheets by ultrasonication and solar light irradiation. The as-prepared 4g-G nanocomposite was characterized by Fourier transform infrared spectroscopy, UV-vis spectroscopy, Scanning transmission electron microscopy, Scanning electron microscopy with energy dispersive X-ray spectrometry, and X-ray diffraction techniques. The photocatalytic activities of the Ag-G nanocomposite were evaluated by the degradation of methylene blue (MB) and methylene orange (MO) in an aqueous medium under sunlight irradiation. The photocatalytic activity of Ag-G nanocomposite for the degradation of MB (k = 0.0163283 min(-1)) > MO (k=0.0140985 min(-1)), due to the anchoring of Ag nanoparticles on the graphene sheets and thiazine ring of MB is more susceptible to photodegradation than the azo bond of MO. This ecofriendly and green reduction method avoids the use of toxic reagents, and it might be useful for biocompatible materials in the future engineering applications. (C) 2016 Elsevier B.V. All rights reserved.

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

 

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Access to 1,3-oxazine-2,4-diones/1,3-thiazine-2,4-diones via organocatalytic CO2/COS incorporation into allenamides

Organocatalyzed [4 + 2] annulation of CO2/COS with allenamides is firstly reported to synthesize 1,3-oxazine-2,4-diones and 1,3-thiazine-2,4-diones in moderate to excellent yields under mild reaction conditions. The catalytic potential of a series of Lewis base CO2 and COS adducts are particularly noted for this process, which features high regio- and chemo-selectivity, step-economy, facile scalability, and easy product derivatization. This study offers the potential for the application of organocatalytic systems for CO2 and COS chemical transformation.

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

 

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Crystal structure of methyl 1-allyl-4-methyl-1H-benzo[c][1,2]thiazine-3-carboxylate 2,2-dioxide

In the title compound, C14H15NO4S, the dihydrothiazine ring adopts a distorted sofa conformation with the S atom displaced from the mean plane through the N and C ring atoms by 0.767 (1) angstrom. The allyl substituent (C-C=C) is inclined to this mean plane by 78.5 (7)degrees and the acetate group [C(=O)-O-C] by 66.5 (3)degrees. In the crystal, molecules are linked by C-H center dot center dot center dot pi interactions forming chains propagating along the a-axis direction.

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

 

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Synthesis, spectroscopic structure identification, X-ray study and anticancer activities of new angularly fused quinobenzothiazines

Synthesis of 16 new tetracyclic angularly fused azaphenothiazines, 8-, 9- and 10-substituted quinobenzo1,4-thiazines (benzo[a]-3-azaphenothiazines) was based on the reactions of dichlorodiquinolinyl disulfide and diquinodithiin with substituted anilines. Whereas the reactions with p-fiuoroaniline and p-methylthioaniline led to only one product, the reaction with m-triflouromethylaniline led to isomeric compounds. The obtained 8-10-substituted 12H-quinobenzothiazines were further transformed into 12 substituted derivatives through allcylation of the thiazine nitrogen atom. The structure analysis was based on 1D and 2D NMR (NOESY, COSY, HSQC and HMBC) spectra which enabled to distinguish the isomers and to exclude retro-Smiles rearrangement and the azine nitrogen atom alkylation pathways. This supposition was fully confirmed by X-ray analysis showing the quinobenzothiazine system to be folded and the substituent at the thiazine nitrogen atom in an equatorial position. Some compounds exhibited anticancer activity against MCF-7, MDA-MB-231 and SNB-19 cell lines similar to a reference drug cisplatin. The structure-activity relationship of the compounds were discussed. (C) 2016 Elsevier B.V. All rights reserved.

This is the end of this tutorial post, and I hope it has helped your research about 10297-73-1. Category: thiazines.

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

 

Discover the magic of the C9H10O3S

This is the end of this tutorial post, and I hope it has helped your research about 10297-73-1. Category: thiazines.

Research speed reading in 2021. Healthcare careers for chemists are once again largely based in laboratories, although increasingly there is opportunity to work at the point of care, helping with patient investigation. , Category: thiazines, 10297-73-1, Name is 4′-(Methylsulfonyl)acetophenone, molecular formula is C9H10O3S, belongs to thiazines compound. In a document, author is Pluta, K., introduce the new discover.

Synthesis, spectroscopic structure identification, X-ray study and anticancer activities of new angularly fused quinobenzothiazines

Synthesis of 16 new tetracyclic angularly fused azaphenothiazines, 8-, 9- and 10-substituted quinobenzo1,4-thiazines (benzo[a]-3-azaphenothiazines) was based on the reactions of dichlorodiquinolinyl disulfide and diquinodithiin with substituted anilines. Whereas the reactions with p-fiuoroaniline and p-methylthioaniline led to only one product, the reaction with m-triflouromethylaniline led to isomeric compounds. The obtained 8-10-substituted 12H-quinobenzothiazines were further transformed into 12 substituted derivatives through allcylation of the thiazine nitrogen atom. The structure analysis was based on 1D and 2D NMR (NOESY, COSY, HSQC and HMBC) spectra which enabled to distinguish the isomers and to exclude retro-Smiles rearrangement and the azine nitrogen atom alkylation pathways. This supposition was fully confirmed by X-ray analysis showing the quinobenzothiazine system to be folded and the substituent at the thiazine nitrogen atom in an equatorial position. Some compounds exhibited anticancer activity against MCF-7, MDA-MB-231 and SNB-19 cell lines similar to a reference drug cisplatin. The structure-activity relationship of the compounds were discussed. (C) 2016 Elsevier B.V. All rights reserved.

This is the end of this tutorial post, and I hope it has helped your research about 10297-73-1. Category: thiazines.

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

 

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Synthesis and biological evaluation of coumarin clubbed thiazines scaffolds as antimicrobial and antioxidant

A new series of 4-methyl-6-nitro-2-oxo-2H-chroman-7yl-2-(4-(4-fluorophenyl)-6-phenyl-2H-1,3-thiazin-2-yl-amino)acetates 5a-j were synthesized from 6-nitro-4-methyl coumarinyl chloroacetate (5) and 2-amino thiazines (IIIa-j). The structure of the final compounds was adequately confirmed via spectroscopic techniques (IR, H-1 NMR, C-13 NMR, Mass) and characterization of physical properties. Final compounds were screened for their antimicrobial, antitubercular, and antioxidant activities. Compounds 5c and 5h found to have antibacterial potency against E. coli with MIC values 50 mu g/mL compared to standard drugs. Compound 5d demonstrated better antifungal potency (MIC = 200 mu g/mL) against C. albicans when compared with griseofulvin. Compounds 5b and 5h found to be encouraging antitubercular (MIC = 62.5 mu g/mL with 98-99% inhibition) against M. tuberculosis H(37)Rv. The newly synthesized 5h and 5b were appeared to have high radical scavenging efficacies as 33.99 +/- 0.301 and 35.35 +/- 0.470 mu g/mL +/- SD of IC50 values, respectively, in DPPH and ABTS bioassay.

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

 

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Access to 1,3-oxazine-2,4-diones/1,3-thiazine-2,4-diones via organocatalytic CO2/COS incorporation into allenamides

Organocatalyzed [4 + 2] annulation of CO2/COS with allenamides is firstly reported to synthesize 1,3-oxazine-2,4-diones and 1,3-thiazine-2,4-diones in moderate to excellent yields under mild reaction conditions. The catalytic potential of a series of Lewis base CO2 and COS adducts are particularly noted for this process, which features high regio- and chemo-selectivity, step-economy, facile scalability, and easy product derivatization. This study offers the potential for the application of organocatalytic systems for CO2 and COS chemical transformation.

Related Products of 10297-73-1, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 10297-73-1 is helpful to your research.

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