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

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Scandium-Catalyzed para-Selective Alkylation of Aromatic Amines with Alkenes

An efficient para-alkylation of primary and secondary anilines with a variety of sterically encumbered alkenes using a simple beta-diketiminato scandium catalyst is reported. This protocol features 100% atom economy, excellent chemo- and regioselectivity, broad substrate scope, and good functional group tolerance. Mechanistic studies disclosed that the reaction probably proceeded via a tandem hydroamination/Hofmann-Martius rearrangement.

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

 

More research is needed about 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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BENZOXAZINES, BENZOTHIAZINES, AND RELATED COMPOUNDS HAVING NOS INHIBITORY ACTIVITY

The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions

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

 

Awesome Chemistry Experiments For 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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7-fused 2-(piperazinoalkyl) indole derivatives, intermediates and compositions thereof

Pharmacologically active compounds having anti-allergic properties corresponding to the formula I STR1 which can be mono- or disubstituted in the phenyl ring and their acid addition salts and/or S-mono- or dioxides of sulfur-containing compounds of the formula I are described, together with processes and intermediates for their preparation.

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

 

Top Picks: new discover of 3080-99-7

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A review on synthesis of benzothiazine analogues

Scientific advances mainly involves the development of new and highly reactive compounds. Nitrogen and sulphur containing benzothiazines forms highly active heterocyclic agents. Benzothiazines are prominent class of heterocyclic compound. Many studies have been done in the development of benzothiazine analogues. Microwave assisted synthesis, regioselective techniques and other methods are also used for benzothiazine synthesis. Various methods have been developed for the synthesis of benzothiazine derivatives. Benzothiazines exhibits numerous therapeutic activities like anti-HIV, calcium antagonistic, anti-serotinin, analgesic, anti-mycobacterial anti-microbial, anti-oxidant, anti-rheumatic, anti-inflammatory, anti-hypertensive ,calcium channel blocker, anti-malarial, potassium channel opener, cardiovascular, anthelmintic, neuroprotective, aldose reductase inhibitor, herbicidal, pesticidal etc. This has raised the necessity to explore novel benzothiazine derivatives which can significantly contribute to the development of therapeutically active agents. And the newer development of novel benzothiazines derivatives also involves the same characteristic features and also contribute various activities.

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

 

Final Thoughts on Chemistry for 3080-99-7

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ORGANOMETALLIC INDUCED SELF-CONDENSATION OF CARBOXAMIDES

N,N-Disubstituted carboxamides containing alpha-hydrogen atoms undergo self-condensation reaction simply on treatment with Grignard reagents or n-BuLi in THF at room temp.The reaction is considerably influenced by steric hindrance at the alpha-carbon and the condensing agent utilized.A possible Claisen-type mechanism is also reported.

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

 

More research is needed about 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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TRICYCLIC INDOLE MCL-1 INHIBITORS AND USES THEREOF

The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.

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

 

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An efficient synthesis of benzene fused six-, seven- and eight-membered rings containing nitrogen and sulfur by benzyne ring closure reaction

3,4-Dihydro-2-H-benzo[1,4]thiazines (3a-c), 2,3,4,5-tetrahydro[b]-[1,4] thiazapines (3d-f) and 2,3,4,5-tetrahydro-2H-benzo[b][1,4]thiazocines (3g-i) were prepared by the cyclization of the respective 2-bromophenylsulfanyl derivatives of ethylamine (1a-c), propylamine (2d-f) and butylamine (2g-i).

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

 

Extracurricular laboratory:new discovery of 3080-99-7

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1-PROPANOL AND 1-PROPYLAMINE DERIVATIVES AND THEIR USE AS GLUCOCORTICOID LIGANDS

Compounds of Formula (I) wherein R1, R2 R3, R4, R5, R6, and X are as defiend herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocoricoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

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

 

Top Picks: new discover of 3,4-Dihydro-2H-benzo[b][1,4]thiazine

The design and synthesis of related molecules that are more effective, more selective, and less toxic than aspirin are important objectives of biomedical research.Keep reading other articles of 3,4-Dihydro-2H-benzo[b][1,4]thiazine!Electric Literature of 3080-99-7

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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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Design of Gut-Restricted Thiazolidine Agonists of G Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5)

Bile acid signaling and metabolism in the gastrointestinal tract have wide-ranging influences on systemic disease. G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is one of the major effectors in bile acid sensing, with demonstrated influence on metabolic, inflammatory, and proliferative processes. The pharmacologic utility of TGR5 agonists has been limited by systemic target-related effects such as excessive gallbladder filling and blockade of gallbladder emptying. Gut-restricted TGR5 agonists, however, have the potential to avoid these side effects and consequently be developed into drugs with acceptable safety profiles. We describe the discovery and optimization of a series of gut-restricted TGR5 agonists that elicit a potent response in mice, with minimal gallbladder-related effects. The series includes 12 (TGR5 EC50: human, 143 nM; mouse, 1.2 nM), a compound with minimal systemic availability that may have therapeutic value to patients with type 2 diabetes mellitus, nonalcoholic steatohepatitis, or inflammatory bowel disease.

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