Brief introduction of Thiazolidin-2-one

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Synthesis and evaluation of thiazolidine-2,4-dione/benzazole derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B): Antihyperglycemic activity with molecular docking study

This work presents the synthesis of two hybrid compounds (1 and 2) with thiazolidine-2,4-dione structure as a central scaffold which were further screened in combo (in vitro as PTP-1B inhibitors, in vivo antihyperglycemic activity, in silico toxicological profile and molecular docking). Compound 1 was tested in the enzymatic assay showing an IC50 = 9.6 ¡À 0.5 muM and compound 2 showed about a 50% of inhibition of PTP-1B at 20 muM. Therefore, compound 1 was chosen to test its antihyperglycemic effect in a rat model for non-insulin-dependent diabetes mellitus (NIDDM), which was determined at 50 mg/kg in a single dose. The results indicated that compound showed a significant decrease of plasma glucose levels that reached 34%, after a 7 h post-administration. Molecular docking was employed to study the inhibitory properties of thiazolidine-2,4-dione derivatives against Protein Tyrosine Phosphatase 1B (PDB ID: 1c83). Concerning to the two binding sites in this enzyme (sites A and B), compound 1 has shown the best docking score, which indicates the highest affinity. Finally, compounds 1 and 2 have demonstrated an in silico satisfactory pharmacokinetic profile. This shows that it could be a very good candidate or leader for new series of compounds with this central scaffold.

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Electric Literature of 7025-19-6, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 7025-19-6, Name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid,introducing its new discovery.

Synthesis of new potential anticancer agents based on 4-thiazolidinone and oleanane scaffolds

The synthesis and evaluation of the anticancer activity of new acylated oximes derivatives of oleanolic acid with 4-thiazolidinone-3(5)-carboxylic acid moieties were described. Newly synthesized compounds were elucidated on the basis of elemental analyses and spectral data (IR, 1H, and 13C NMR). Anticancer activity of the tested compounds has been evaluated in vitro at National Cancer Institute (NCI) in which some structure activity relationships (SARs) were discussed. Among the tested compounds, 3-[(2,4-thiazolidinedione-5-ylidene)-carboxyimino] olean-12-en-28-oic acid methyl ester (IVm) was superior to other related compounds with mean values of pGI50 = 5.51/5.57, pTGI = 5.09/5.13, and pLC50 = 4.62/4.64, low toxicity and moderate activity level in vivo hollow fiber assay. Springer Science+Business Media, LLC 2011.

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Related Products of 185137-29-5, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.185137-29-5, Name is (S)-4-Phenylthiazolidine-2-thione, molecular formula is C9H9NS2. In a Article£¬once mentioned of 185137-29-5

Kinetic resolution of N-acyl-thiolactams via catalytic enantioselective deacylation

Methanolysis of N-acyl-thiazolidin-2-thiones and -oxazolidin-2-thiones in the presence of acyl transfer catalyst benzotetramisole (BTM) proceeds in a highly enantioselective fashion thus enabling kinetic resolution of these substrates.

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Application of 19771-63-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19771-63-2, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S. In a Article£¬once mentioned of 19771-63-2

Preparation and characterization of new In(III), Re(III), and Re(V) complexes with thenoyltrifluoroacetone and some bidentate heterocyclic ligands

New In(III), Re(III) and Re(V) complexes with the thenoyltrifluoroacetone ligand (HTTA) of the general formulae [In -(TTA)(H2O)4]SO4, [Re(TTA)n(H2O)x]Cl3-n and [ReO(TTAn-(H2O)x]Cl3-n (where n and x refer to the number of [TTA]- moieties and H2O molecules, respectively) have been prepared and characterized by spectroscopy, thermogravimetry, elemental analyses and X-ray diffraction. The charge densities on the ligand atoms were calculated via CNDO-SCF calculations. The newly prepared complexes [In(TTA)(H2O)4]SO2 and [ReO(TTA)(H2O)2]CL2 were employed as precursors for the synthesis of the mixed-ligand complexes [In(TTA)(HOCTA)2], [In(TTA)(TZT)2] and [ReO(TTA)(HOTCA)]Cl using R(-)-2-oxothiazolidine 4-carboxylicacid (H2OTCA) and 1H-1,2,4-triazole-3-thiol (H2TZT) as ligands. The synthesized mixed-ligand complexes were characterized by the conventional physical and chemical methods of analysis applied earlier for the characterization of the precursors. The investigated complexes are soluble in water, ethanol and acetonitrile, insoluble in non-polar solvents and could be of potential use for clinical studies. The antibacterial activity of the investigated complexes has been tested and evaluated.

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More research is needed about 7025-19-6

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7025-19-6, Name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid, belongs to thiazolidine compound, is a common compound. Computed Properties of C6H7NO3S2In an article, once mentioned the new application about 7025-19-6.

INHIBITORS OF EPSTEIN BARR VIRUS NUCLEAR ANTIGEN 1

The invention relates to a high throughput assay and methods for detecting inhibitors. The invention also relates to the inhibitors identified by the assay methods, and methods of using the inhibitors to treat and prevent disease.

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Extended knowledge of 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

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Sensitized Room Temperature Biacetyl Phosphorescence via Molecular Organization

Room temperature biacetyl phosphorescence enhanced via molecular organization is observed for many aromatic compounds.Micelles composed of sodium dodecyl sulfate(SDS) and hosts such as beta-cyclodextrin(beta-CD) are used to enhance the energy transfer reaction by organizing the reactants in close proximity to one another.The triplet-triplet energy transfer of several polynuclear aromatics, nitrogen heterocyclics, and heavy-atom-substituted species to biacetyl was evaluated.Both SDS and beta-CD were found to provide a superior medium for production of sensitized biacetylphosphorescence than found with homogenous solution.Typically,limits of detection of 1x 10-8 to 10-9 M in SDS and 1 x 10-7 M in beta-CD were obtained.The sensitivities of the methods are dependent on the solubility of the donor in SDS, the ability of the donor to fit into the beta-cyclodextrin cavity, and the background signal produced by the biacetyl blank solution.

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Properties and Exciting Facts About (R)-Ethyl thiazolidine-4-carboxylate hydrochloride

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 86028-91-3, name is (R)-Ethyl thiazolidine-4-carboxylate hydrochloride, introducing its new discovery. Product Details of 86028-91-3

Synthesis of heterocyclic platelet activating factor analogues

The synthesis of heterocyclic analogues of the platelet activating factor is described. The preparation starts with acylating rac-tetrahydro-1,3-thiazine-4-carboxylic acid ethyl ester, with palmitoyl chloride to form the amide linkage. Following ester reduction, the phosphocholine part is introduced via 2-chloro-2-oxo-1,3,2-dioxaphospholane and subsequent ring opening with trimethylamine under pressure. Furthermore, the related L-thiazolidine analogue is prepared using the same procedure. In addition the sulfinyl and sulfonyl derivatives of this compound are obtained by oxidation with 3-chloro-perbencoic acid. From one sulfinyl intermediate the diastereomeres are separated and their conformations are determinated by 13C-NMR spectroscopy.

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A new application about 5908-62-3

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Reference of 5908-62-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.5908-62-3, Name is 1,1-Dioxo-isothiazolidine, molecular formula is C3H7NO2S. In a Patent£¬once mentioned of 5908-62-3

7, 9-NITROGEN RADICAL-4-OXO-4H-PYRIDO[L,2-A]PYRIMIDINE-2-CARBOXYLIC ACID BENZYLAMIDE ANTI-VIRALS

The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided

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Arylidenes of Quinolin-2-one scaffold as Erlotinib analogues with activities against leukemia through inhibition of EGFR TK/ STAT-3 pathways

A new series of 6-substiuted-4-(2-(4-substituted-benzylidene)hydrazinyl)quinolin-2(1H)-one derivatives have been designed and synthesized. The structure of the synthesized compounds was proved by 1H NMR, 13C NMR, 2D NMR, mass and elemental analyses. The target compounds were evaluated for their in vitro cytotoxic activity against 60 cancer cell lines according to NCI protocol. Consequently, the most active compounds were further examined against the most sensitive leukemia RPMI-8226 and on healthy cell lines. 6-Chloro-derivative was the most active one; with IC50 = 15.72 ¡À 1.21 and 46.05 ¡À 2.36 muM against RPMI-8226 and normal cell lines, respectively. Also, it showed a remarkable inhibitory activity compared to gefitinib on the EGFR TK mutant, wild and on H-RAS in addition to STAT-3 with IC50 = 695.49 ¡À 21.8, 263.15 ¡À 15.13, 10.61 ¡À 0.27 and 1.753 ¡À 0.81 nM, respectively. Cell cycle analysis of RPMI-8226 cells treated with the 6-chloro-derivative showed cell cycle arrest at G2/M phase (supported by Caspases-3,8, BAX and Bcl-2 studies) with a significant pro-apoptotic activity as indicated by annexin V-FITC staining. Moreover, the docking studies ROCS analysis and Tanimoto scores supported the results. The study illustrated the effect of several factors on compounds activity.

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Properties and Exciting Facts About 185137-29-5

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Related Products of 185137-29-5, 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, 185137-29-5, molcular formula is C9H9NS2, introducing its new discovery.

Oxazolidine-2-thiones and thiazolidine-2-thiones as nucleophiles in intermolecular michael additions

Conjugate addition of thiazolidinethiones and oxazolidinethiones to N-crotonylthiazolidinethiones and -oxazolidinethiones was observed in the presence of excess triethylamine in dichloromethane. The addition takes place by the nitrogen of the heterocycle with high diastereoselectivity. It was observed that the stereoselective addition occurs on the anti-s-cis conformation of the N-enoyl sulfur-containing heterocycle.

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