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Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists

4-Phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists are reported. Several 4-phenoxynicotinamide derivatives were found to activate human and mouse TGR5 (hTGR5 and mTGR5) with EC50 values in the low nanomolar range. Compound 23g, with an EC50 value of 0.72 nM on hTGR5 and an EC 50 value of 6.2 nM on mTGR5, was selected for further in vivo efficacy studies. This compound exhibited a significant dose-dependent glucagon-like peptide-1 (GLP-1) secretion effect. A single oral dose of 23g (50 mg/kg) significantly reduced blood glucose levels in db/db mice and caused a 49% reduction in the area under the blood glucose curve (AUC)0-120min following an oral glucose tolerance test (OGTT) in imprinting control region (ICR) mice. However, 23g stimulated gallbladder filling, which might result in side effects to the gallbladder.

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

 

Discovery of 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid

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272437-84-0, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 272437-84-0, name is 3-Oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid. In an article£¬Which mentioned a new discovery about 272437-84-0

Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains

We have previously reported a novel class of tetrahydroindazoles that display potency against a variety of Gram-positive and Gram-negative bacteria, potentially via interaction with type II bacterial topoisomerases. Herein are reported SAR investigations of this new series. Several compounds possessing broad-spectrum potency were prepared. Further, these compounds exhibit activity against multidrug-resistant Gram-positive microorganisms equivalent to that against susceptible strains.

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

 

Discovery of 3080-99-7

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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. 3080-99-7

SPIRO-CYCLIC BETA-AMINO ACID DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEASES AND TNF-ALPHA CONVERTING ENZYME (TACE)

The present application describes novel spiro-cyclic beta-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-alpha converting enzyme (TACE), and/or aggrecanase inhibitors.

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

 

Simple exploration of 3080-99-7

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Chemoselective Deprotection of Sulfonamides under Acidic Conditions: Scope, Sulfonyl Group Migration, and Synthetic Applications

Chemoselective acidic hydrolysis of sulfonamides with trifluoromethanesulfonic acid has been evaluated as a deprotection method and further extended to more complex synthetic applications. In contrast to conventional troublesome sulfonamide hydrolysis, a near-stoichiometric amount of acid was found to be sufficient to bring about efficient deprotection of various neutral or electron-deficient N-arylsulfonamides, whereas electron-rich substrates provided sulfonyl group migration products. The deprotection method developed is fully selective for N-arylsulfonamides, and the possibility to discriminate among various different sulfonamides is demonstrated.

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

 

A new application about 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7)

The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

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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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TETRAHYDROQUINOLINE SUBSTITUTED HYDROXAMIC ACIDS AS SELECTIVE HISTONE DEACETYLASE 6 INHIBITORS

Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.

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

 

Can You Really Do Chemisty Experiments About 3,4-Dihydro-2H-benzo[b][1,4]thiazine

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3080-99-7, In heterogeneous catalysis, the catalyst is in a different phase from the reactants. At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 3080-99-7, name is 3,4-Dihydro-2H-benzo[b][1,4]thiazine. In an article£¬Which mentioned a new discovery about 3080-99-7

An efficient method for the N-formylation of amines under catalyst- and additive-free conditions

A simple catalyst- and additive-free method for the N-formylation of amines has been developed. The advantages of this protocol include a wide range of functional group tolerance, high efficiency and a lack of required extra promoters under mild conditions. This convenient strategy will provide a facile synthesis towards N-formamide natural products and pharmaceutical derivatives. A mechanism that involves difluorocarbene is proposed for this reaction.

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

 

Awesome and Easy Science Experiments about 188614-01-9

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188614-01-9, 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, 188614-01-9, molcular formula is C10H9NO3S, introducing its new discovery.

ANTIBACTERIAL COMPOUNDS

Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man

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

 

New explortion of 272437-84-0

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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

 

Awesome and Easy Science Experiments about 1910-85-6

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1910-85-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1910-85-6, Name is 1-Chloro-10H-phenothiazine, molecular formula is C12H8ClNS. In a Article, authors is Self, Jennifer L.£¬once mentioned of 1910-85-6

REACTION OF CHLORO DERIVATIVES OF 10-BENZYL- AND 10-(4′-FLUOROBENZYL)PHENOTHIAZINES WITH NITRILES AND AMINES UNDER ARYNE-FORMING CONDITIONS

2-Chloro-10-benzylphenothiazine (1) and 2-chloro-10-(4′-fluorobenzyl)phenothiazine (2) react with aliphatic nitriles (3 and 4) and LDA to yield typical 2-substituted aryne products (9a,b and 9g,h, respectively).However, treatment of 1 with aromatic nitriles (5-8) and LDA supplies 2-(arylmethyl)-1-cyano rearranged nitriles (10c-f), whereas 2, when treated similarly, affords both rearranged nitriles (10i-l) and typical 2-arylated nitrile products (9i-j).An explanation in terms of the effect of substituents on the competing aryne and tandem addition-rearrangement pathways is presented.The crystal structure of one of the rearranged 1-cyanophenothiazines (10c) was obtained and reveals that the molecule adopts the “extra” conformation in which the 10-benzyl group is in the pseudo axial position.The reaction of 1 and 2 with various lithium amides in the corresponding free amine solvents gives the corresponding 2-aminated products (11) and (12) in excellent yields.Both 1-chloro-10-benzylphenothiazine (18) and 1 supply the same product, 10-benzyl-2-N,N-diisopropylaminophenothiazine (11a), when made to react with LDA in diisopropylamine solvent, indicating that each of these reactions proceeds via the same aryne intermediate, and not through the SRN1 mechanism.

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