Extracurricular laboratory:new discovery of 111248-89-6

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NOVEL NAPHTHYRIDINES AND ISOQUINOLINES AND THEIR USE AS CDK8/19 INHIBITORS

The present invention relates to naphthyridine and isoquinoline compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of CDK8/19, and for the treatment of CDK8/19-related disorders.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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SUBSTITUTED DIHYDROTHIENOPYRIMIDINES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS

The present invention relates to novel substituted dihydrothienopyrimidines with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Synthesis, Identification, and Structure-Activity Relationship Analysis of GATA4 and NKX2-5 Protein-Protein Interaction Modulators

Transcription factors GATA4 and NKX2-5 directly interact and synergistically activate several cardiac genes and stretch-induced cardiomyocyte hypertrophy. Previously, we identified phenylisoxazole carboxamide 1 as a hit compound, which inhibited the GATA4-NKX2-5 transcriptional synergy. Here, the chemical space around the molecular structure of 1 was explored by synthesizing and characterizing 220 derivatives and structurally related compounds. In addition to the synergistic transcriptional activation, selected compounds were evaluated for their effects on transcriptional activities of GATA4 and NKX2-5 individually as well as potential cytotoxicity. The structure-activity relationship (SAR) analysis revealed that the aromatic isoxazole substituent in the southern part regulates the inhibition of GATA4-NKX2-5 transcriptional synergy. Moreover, inhibition of GATA4 transcriptional activity correlated with the reduced cell viability. In summary, comprehensive SAR analysis accompanied by data analysis successfully identified potent and selective inhibitors of GATA4-NKX2-5 transcriptional synergy and revealed structural features important for it.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Reference of 27148-03-4, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 27148-03-4, Name is Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide,introducing its new discovery.

Synthesis of 1,2,3-Benzothiadiazine-1,1 -dioxide Derivatives and their Pharmacological Properties

Formation of 4-(Sub)-amino-1,2,3-benzothiadiazine-1,1-dioxide was established by earlier reported base catalysed ring expansion reaction. Products thus obtained, were stable in aqueous alkaline and acidic medium and on alkylation/acylation furnished 4-amino derivative (4, 5) exclusively, instead of 2-N-derivative (3). Preliminary pharmacological screening was done and the results were positive.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

Can You Really Do Chemisty Experiments About Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 27148-03-4

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A comparative study of the coordination of saccharinate, thiosaccharinate and benzisothiozolinate ligands to cyclometalated [Pd(Me2NCH2C6H4-kappa2N,C)(mu-Cl)]2: Molecular structures of [Pd(Me2NCH2C6H4-kappa2N,C)(mu-X)]2 (X?=?sac, bit and tsac) and [Pd(Me2NCH2C6H4-kappa2N,C)Cl(ampyH-kappa1N)] (ampyH?=?2-amino-3-methylpyridine)

Reactions of [Pd(Me2NCH2C6H4-kappa2N,C)(mu-Cl)]2 with two equivalents of sodium saccharinate (Nasac), thiosaccharin (Htsac) or sodium benzisothiozolinate (Nabit) results in the stepwise substitution of the bridging halides to form sequentially [Pd2(Me2NCH2C6H4-kappa2N,C)2(mu-Cl)(mu-X)] (X = sac, tsac) and [Pd(Me2NCH2C6H4-kappa2N,C)(mu-X)]2 (X = sac, tsac, bit). The molecular structures of all three disubstituted complexes are reported. In each the two metalated ligands bind in a chelate manner adopting a relative anti conformation, while the new ligands bridge the two palladium atoms adopting a relative cis conformation. The local conformation about each palladium differs with small ligand changes. Thus in the sac and bit complexes all nitrogens lie trans to one another, in the tsac complex they are cis. Conformational changes also lead to large differences in the non-bonded Pd?Pd distance which range over 0.5 A. Treatment of [Pd(Me2NCH2C6H4-kappa2N,C)(mu-Cl)]2 with two equivalents of 2-amino-3-methylpyridine (ampyH) in the presence of NEt3 affords mononuclear [PdCl(Me2NCH2C6H4-kappa2N,C)(ampyH-kappa1N)] as a result of ?bridge-splitting?, the ampyH ligand binding through the pyridyl-nitrogen and lying approximately perpendicular to the PdCClN2 plane as shown by a crystallographic study.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS

The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Mono and polynuclear silver(I) complexes with thiosaccharine and triphenylphosphine or 2,2?-bipyridine. Synthesis, spectroscopic and structural characterization

Reaction of Ag6(tsac)6 (tsac- = thiosaccharinate anion) with PPh3 and 2,2?-bipyridine (bipy) ligands give rise to three new silver-thiosaccharinate complexes, [Ag(tsac)(PPh3)3], [Ag4(tsac)4(PPh3)3], and [Ag2(tsac)2(bipy)2]. Their crystal structures established by single-crystal X-ray diffraction and IR spectroscopic characterizations are reported here. In each complex a singular coordination mode for the thiosaccharinate ligands is observed. The most important features of the different coordination modes of the thionates are discussed.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

The important role of Benzo[d]isothiazole

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Reference of 272-16-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.272-16-2, Name is Benzo[d]isothiazole, molecular formula is C7H5NS. In a Article£¬once mentioned of 272-16-2

Reaction of Benzyne with 1,2,5-Thiadiazoles and 2,1-Benzisothiazoles

1,2,5-Thiadiazoles react with benzyne to give 1,2-benzisothiazole derivatives. 3.4-Diphenyl-1,2,5-selenadiazole with benzyne likewise affords 3-phenyl-1,2-benzisoselenazole, contrary to a previous report.Some reactions of 3-(8-cyano-1-naphthyl)-1,2-benzisothiazole are described.The reaction of benzyne with 3-amino-2,1-benzisothiazole afforded N-phenylated products, including N-phenyl-anthranonitrile.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

The important role of 4576-90-3

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3-Aryl-5-isothiazolecarboxylic acids and related compounds used to lower uric acid levels

3-Phenyl (or meta or para-substituted phenyl)-4-permissibly substituted-5-isothiazolecarboxylic acids, salts, esters and simple amides, used to lower uric acid levels in mammals.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.Formula: C7H5NS, Name is Benzo[d]isothiazole, molecular formula is C7H5NS, Formula: C7H5NS. In a Article, authors is Lawson, Alexander J.£¬once mentioned of Formula: C7H5NS

THERMAL FISSION OF HYDROXYLAMINE DERIVATIVES WITH NEIGHBOURING-GROUP-PARTICIPATION BY THIOETHER FUNCTIONS: PREPARATION OF 1,2-BENZISOTHIAZOLES

Some of the factors influencing the preparation of 1,2-benzisothiazoles from 2-(alkylthio)phenyl-substituted oximes are discussed.Good yields of 3-aryl-1,2-benzisothiazoles 4 may be obtained from readily available precursors.Reaction takes place under particularly mild conditions when a t-butylthio function is situated anti to the leaving group at oxime-nitrogen and S-N overlap is not restricted by ring-strain in the transition-state.The corresponding N-methyl-hydroxamic acid derivatives 2 give good yields of 2-methyl-1,2-benzisothiazol-3(2H)-one 13 only when a t-butylthio substituent is present, e.g. in 2f.The ethylthio- and i-propylthio-analogues 2d and 2e give the vinylthioethers 12, while the methylthio derivatives 2a-c undergo a novel rearrangement to “Pummerer” esters.The preparation of the polycyclic compounds fluoreno<9,9a,1-cd>-1,2 thiazole 7 and 2,2′-bi(2H-fluoreno<9,9a,1-de>-1,3-thiazine) 8 is described.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com