Heterocyclic Building Blocks-Thiazolidine

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 2421-28-5, Name is Benzophenone-3,3′,4,4′-tetracarboxylic dianhydride, molecular formula is C17H6O7, belongs to thiazolidines compound, is a common compound. In a patnet, author is Ying, Jun, once mentioned the new application about 2421-28-5, Category: thiazolidines.

Base-Promoted Sulfur-Mediated Carbonylative Cyclization of Propargylic Amines

A tBuOK-mediated carbonylative cyclization of propargylic amines with elemental sulfur has been developed. With benzene-1,3,5-triyl triformate (TFBen) as a convenient CO surrogate, various substituted 1,3-thiazolidin-2-ones were produced in good to excellent yields.

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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 593-85-1, Name is guanidinecarbonate, molecular formula is C3H12N6O3. In an article, author is Brahmbhatt, Harshad,once mentioned of 593-85-1, Name: guanidinecarbonate.

Synthesis, Characterization, Antibacterial and Antioxidant Potency of N-Substituted-2-Sulfanylidene-1,3-Thiazolidin-4-one Derivatives and QSAR Study

Background: Rhodanine is known for its potential and important role in the medicinal chemistry since its derivatives exhibit a wide range of pharmacological activities such as antibacterial, antifungal, antidiabetic, antitubercular, anti-HIV, antiparasitic, antioxidant, anticancer, antiproliferative and anthelmintic agents. Objectives: Since N-substituted rhodanine synthons are rarely commercially available, it is desirable to develop a straightforward synthetic approach for the synthesis of these key building blocks. The objective was to synthesize a series of rhodanine derivatives and to investigate their antimicrobial and antioxidant activity. Also, in order to obtain an insight into their structure-activity relationship, QSAR studies on the antioxidant activity were performed. Methods: H-1 and C-13 FTNMR spectra were recorded on Bruker Avance 600 MHz NMR Spectrometer, mass analysis was carried out on ESI+ mode by LC-MS/MS API 2000. 2,2-Diphenyl-1-picrylhydrazyl radical scavenging activity (% DPPH) was determined in dimethylsulfoxide (DMSO) as a solvent. The antibacterial activity was assessed against Bacillus subtilis, Staphylococcus aureus (Gram positive) and Escherichia coli, Pseudomonas aeruginosa (Gram negative) bacteria in terms of the minimum inhibitory concentrations (MICs) by a modified broth microdilution method. Results: A series of N-substituted-2-sulfanylidene-1,3-thiazolidin-4-ones were synthesized and characterized by H-1 NMR, C-13 NMR, FTIR, GC MS, LCMS/ MS and C,H,N,S elemental analysis. Most of the synthesized compounds showed moderate to excellent antibacterial activity (MIC values from 125 mu g/ml to 15.62 mu g/mL) and DPPH scavenging activity (from 3.60% to 94.40%). Compound 2-thioxo-3-(4-(trifluoromethyl)-phenyl)thiazolidin-4-one showed the most potent activity against Escherichia coli (3.125 mu g/mL), equivalent to antibiotic Amikacin sulphate and against Staphylococcus aureus (0.097 mu g/ml), 100 times superior then antibiotic Amikacin sulphate. It has also shown a potent antioxidant activity (95% DPPH scavenging). Two best QSAR models, obtained by GETAWAY descriptor R7p(+), Balabans molecular connectivity topological index and Narumi harmonic topological index (HNar), suggest that the enhanced antioxidant activity is related to the presence of pairs of atoms higher polarizability at the topological distance 7, substituted benzene ring and longer saturated aliphatic chain in N-substituents. Conclusion: A series of novel N-substituted-2-thioxothiazolidin-4-one derivatives were designed, synthesized, characterized and evaluated for their antibacterial and antioxidant activity in vitro. Majority of the compounds showed excellent antibacterial activity compared to ampicillin and few of them have an excellent activity as compared to Chloramphenicol standard antibacterial drug. The QSAR study has clarified the importance of presenting a pairs of atoms higher polarizability, such as Cl and S at the specific distance, as well as the substituted benzene ring and a long saturated aliphatic chain in N-substituents for the enhanced antioxidant activity of 2-sulfanylidene-1,3thiazolidin-4-one derivatives.

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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 137-40-6, Name is Sodiumpropionate. In a document, author is Ulusoy, Seyhan, introducing its new discovery. Recommanded Product: 137-40-6.

Quorum Sensing Inhibitor Activities of Celecoxib Derivatives in Pseudomonas aeruginosa

Background: A series of novel N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)3-( trifluoromethyl)-1H-pyrazol-1-yl] benzene sulfonamides [SGK 318, 319, 320, 324, 327] and N-(3-substitutedaryl/ alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamides[SGK 328, 329, 330, 334, 337] were synthesized and tested for their quorum sensing inhibitor (QSI) capacity using quorum sensing inhibitor selector 1 (QSIS1) bioassay. Findings: QSIS assay revealed that SGK 324, SGK 327 and SGK 330 have the potentials to interfere with QS system in QS inhibitor selector1 (QSIS1) reporter strain. Moreover, these compounds were found to significantly affect QS regulated elastase and biofilm productions in Pseudomonas aeruginosa PA01 strain without affecting its growth. Molecular modeling experiments suggested that SGK 330 fits within the binding site of LasR protein of P. aeruginosa. SGK 324 and 327 also bind LasR provided that they adopt a s-trans/s-cis conformation with respect to the thiourea function. Results and Conclusion: Results of this study indicated that these compounds could be developed as new QS inhibitors without killing the bacteria but as antivirulence compounds to restrict virulence of clinically important human pathogens.

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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Electric Literature of 78-39-7, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 78-39-7, Name is 1,1,1-Triethoxyethane, SMILES is CC(OCC)(OCC)OCC, belongs to thiazolidines compound. In a article, author is Kumar, Harsh, introduce new discover of the category.

Chemical Synthesis, Mechanism of Action and Anticancer Potential of Medicinally Important Thiazolidin-2,4-dione Derivatives: A Review

Thiazolidin-2,4-dione (TZD) possessing an active methylene constitute an important chemical class of compounds for the development of new drugs. So, many scholars have synthesized these derivatives as target molecules and evaluated their biological potential. Currently, some of the TZDs are synthesized to treat human cancers stating high levels of PPAR gamma because it is expected that activation of PPAR gamma arbitrates their anticancer activity because PPAR gamma ligands have recently been established to affect differentiation, cell proliferation and apoptosis of different cell types. In the present review, the synthesis of various derivatives of thiazolidine-2,4-diones, their mechanism of action and anticancer activity have been highlighted.

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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 83237-15-4, Name is 3-(3,5-Di-tert-butyl-1-hydroxy-4-oxocyclohexa-2,5-dien-1-yl)propanoic acid, molecular formula is C17H26O4. In an article, author is Senkardes, Sevil,once mentioned of 83237-15-4, Computed Properties of C17H26O4.

Synthesis of Diflunisal Thiazolidinones as Anticancer Agents

A series of diflunisal 4-thiazolidinones were synthesized. Some selected compounds were determined at one dose towards the full panel of 60 human cancer cell lines by National Cancer Institute. 2′,4′-Difluoro-4-hydroxy-N-[4-oxo-2-(thiophen-2-yl)-1,3-thiazolidin-3-yl]biphenyl-3-carboxamide (4a) demonstrated the most marked effect on K-562 cancer cell line with 58.59 % growth inhibition at 10 mu M. Compound 4a was evaluated in vitro using the MTT colorimetric method against human leukemia cell line K-562 and mouse embryonic fibroblasts cell line NIH-3T3 at different doses for cell viability and growth inhibition. Compound 4a exhibited anticancer activity with IC50 value of 5.2 mu M against K-562 cells and did not display cytotoxicity towards NIH-3T3 cells compared with diflunisal. In addition, this compound could be an interesting prototype as an antiproliferative agent.

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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Chemistry, like all the natural sciences, begins with the direct observation of nature¡ª in this case, of matter.6117-80-2, Name is (Z)-But-2-ene-1,4-diol, SMILES is OC/C=CCO, belongs to thiazolidines compound. In a document, author is Toubal, K., introduce the new discover, COA of Formula: C4H8O2.

Spectroscopic (FT-IR,H-1 and C-13 NMR) characterization and density functional theory calculations for (Z)-5-(4-nitrobenzyliden)-3-N(2-ethoxyphenyl)-2-thioxo-thiazolidin-4-one (ARNO)

In this work, the vibrational spectral analysis is carried out by using FTIR spectroscopy in the range 4000 -400 cm(-1) (2)-5-(4-nitrobenzyliden)-3-N(2-ethoxypheny1)-2-thioxo-thiazolidin-4-one (ARNO) molecule. Theoretical calculations were performed by using density functional theory (DFT) method using 6-31G (d, p) and 6-311G (d, p) basis sets. The results of the calculations were applied to simulated spectra of the title compound, which show excellent agreement with observed spectra. The first order hyperpolarizability and related properties (mu and alpha) for ARNO were also calculated. Stability of the molecule has been analyzed by natural bond orbital (NBO) analysis. Mulliken population analysis on atomic charges of the title compound has been carried out by the same method and basis sets. Finally, molecular electrostatic potential (MEP) and HOMO-LUMO energy levels have been evaluated. (C) 2017 Elsevier B.V. All rights reserved.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 6117-80-2 is helpful to your research. COA of Formula: C4H8O2.

Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Electric Literature of 85-42-7, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 85-42-7, Name is Hexahydroisobenzofuran-1,3-dione, SMILES is O=C1OC(C2CCCCC21)=O, belongs to thiazolidines compound. In a article, author is Mirakmahaleh, Maedeh Saeedi, introduce new discover of the category.

Expedient synthesis of novel antibacterial hydrazono-4-thiazolidinones under catalysis of a natural-based binary ionic liquid

A library of pyran-2H-one-3-ylmethylidene and chromene-2H-one-3-ylmethylidene derivatives of the titled heterocyclic framework was synthesized from 3-acyl-4-hydroxypyran/chromene-2H-one via sequential reaction with thiosemicarbazide and dialkyl acetylenedicarboxylates. The syntheses were carried out under efficient catalysis of a new binary ionic liquid mixture [l-prolinium chloride][1-methylimidazolium-3-sulfonate] in one pot and solvent-free conditions. Calculations based on density functional theory displayed that the barrier energy for interconversion of the two possible diastereomeric isomers of each product is less than the thermal energy of molecules at room temperature, as only one product can be resolved from a given reaction mixture. This seems to be the case for the previously reported hydrazonothiazolidines. The binary ionic liquid mixture melts at near room temperature and can be considered as a solution of HCl in 1:1 mixture of two zwitterionic species. It proved to be more efficient than its constituents in catalyzing the above synthesis in one-pot operation. Some of the synthesized products have shown pronounced antibacterial activities. The ionic liquid is virtually stable in air and moisture, as can be retrieved several times without appreciable decrease in its catalytic activity. Graphic abstract

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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 78-39-7, Name is 1,1,1-Triethoxyethane. In a document, author is Qiang, Zhe, introducing its new discovery. Safety of 1,1,1-Triethoxyethane.

Design and Development of Novel 1,3,5-Triazine-Procaine Derivatives as Protective Agent against Myocardial Ischemia/Reperfusion Injury via Inhibitor of Nuclear Factor-kappa B

The aim of the present study was to determine the protective effect of novel 1,3,5-triazine-procaine derivatives against myocardial ischemia/reperfusion (I/R) injury. Initially, the experiment has been started by the synthesis of procaine, which later got substituted with diverse 1,3,5-triazine derivatives to furnish the final compounds. The target compounds were tested for nuclear factor-kappa B (NF-kappa B) inhibitory activity in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The antioxidant activity of most potent compound 9i was investigated using hydroxyl radical, DPPH, and superoxide anion scavenging assay. Compound 9i was further evaluated for protective effect against myocardial I/R injury on the basis numerous parameters, for example, hemodynamic parameters (left ventricular developed pressure [LVDP], +/- dp/dt_max, coronary flow [CF], and heart rate [HR]), myocardial enzymes (creatine kinase and lactate dehydrogenase), thiobarbituric acid reactive substance (TBARS), oxidative stress (super oxide dismutase [SOD], catalase [CAT], glutathione [GSH], and glutathione peroxidise [GPx]), histopathology, western blots analysis for B-cell lymphoma 2 (Bcl-2), Bcl-2-associated x protein (Bax), lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1), and NF-kappa B in cardiac tissues. Compounds showed significant inhibition of NF-?B transcriptional activity in LPS-stimulated RAW264.7 cells, revealing compound 9i as a most potent derivative. In vitro results showed efficient reduction of reduced hydroxyl radical, DPPH, and superoxide anion by 9i. The level LVDP, +/- dp/dtmax, CF, HR, TBARS, SOD, CAT, GSH, GPx, and damaged cardiac histopathology were completely restored to normal in 9i-treated group, as compared to I/R group. In western blot analysis, the expression of Bax, LOX-1, and NF-kappa B was found to be decreased, while the level of Bcl-2 was found to be increased in 9i-treated group. The procaine-1,3,5-triazine derivatives showed significant cardioprotective action via inhibition of NF-kappa B.

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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 10097-02-6, Name is 2,2-Bis(hydroxymethyl)butyric acid, formurla is C6H12O4. In a document, author is Sigalapalli, Dilep Kumar, introducing its new discovery. Category: thiazolidines.

Novel chromenyl-based 2-iminothiazolidin-4-one derivatives as tubulin polymerization inhibitors: Design, synthesis, biological evaluation and molecular modelling studies

Here-in, we present molecular design, chemical synthesis and evaluation of novel chromenyl-based 2-iminothiazolidin-4-one derivatives as tubulin polymerization inhibitors. The newly synthesized compounds were evaluated for their in vitro cytotoxicities against A549 (lung cancer), MDA-MB-231 and BT-471 (breast cancer), HepG2 (liver cancer) and HCT-116 (colon cancer) cell lines by MTT assay. Among the synthesized compounds, compound 12b showed excellent anticancer activity on MDA-MB-231 cell line with IC50 value of 0.95 +/- 1.88 mu M and was verified to be safe in normal human bronchial epithelial cells (Beas-2B). Apoptosis induced by the lead 12b was observed using morphological observations, AO/EB and DAPI staining procedures. Further, dose-dependent increase in the depolarization of mitochondrial membrane was also observed through JC-1 staining. Annexin V-FITC/PI assay confirmed that 12b induced early apoptosis. Additionally, cell cycle analysis indicated that the MDA-MB-231 cells were arrested at sub-G2/M phase and also inhibited tubulin polymerization with IC50 value of 3.54 +/- 0.2 mM. Molecular docking simulations were employed to identify the important binding modes responsible for the tubulin inhibitory activity, thus supporting their effective anticancer potential. (c) 2020 Published by Elsevier B.V.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 10097-02-6 help many people in the next few years. Category: thiazolidines.

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Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 83237-15-4, Name is 3-(3,5-Di-tert-butyl-1-hydroxy-4-oxocyclohexa-2,5-dien-1-yl)propanoic acid, molecular formula is C17H26O4. In an article, author is de Oliveira Filho, Gevanio Bezerra,once mentioned of 83237-15-4, HPLC of Formula: C17H26O4.

Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi

Chagas disease is one of the most significant health problems in the American continent. benznidazole (BDZ) and nifurtimox (NFX) are the only drugs approved for treatment and exhibit strong side effects and ineffectiveness in the chronic stage, besides different susceptibility among T. cruzi DTUs (Discrete Typing Units). Therefore, new drugs to treat this disease are necessary. Thiazole compounds have been described as potent trypanocidal agents. Here we report the structural planning, synthesis and anti-T cruzi evaluation of a new series of 1,3-thiazoles (7-28), which were designed by placing this heterocycle instead of thiazolidin-4-one ring. The synthesis was conducted in an ultrasonic bath with 2-propanol as solvent at room temperature. By varying substituents attached to the phenyl and thiazole rings, substituents were observed to retain, enhance or greatly increase their anti-T. cruzi activity. In some cases, methyl at position 5 of the thiazole (compounds 9, 12 and 23) increased trypanocidal property. The exchange of phenyl for pyridinyl heterocycle resulted in increased activity, giving rise to the most potent compound against the trypomasigote form (14, IC50trypo = 0.37 mu M). Importantly, these new thiazoles were toxic for trypomastigotes without affecting macrophages and cardiomyoblast viability. The compounds were also evaluated against cruzain, and five of the most active compounds against trypomastigotes (7, 9, 12, 16 and 23) inhibited more than 70% of enzymatic activity at 10 mu M, among which compound 7 had an IC50 in the submicromolar range, suggesting a possible mechanism of action. In addition, examination of T. cruzi cell death showed that compound 14 induces apoptosis. We also examined the activity against intracellular parasites, revealing that compound 14 inhibited T cruzi infection with potency similar to benznidazole. The antiparasitic effect of 14 and benznidazole in combination was also investigated against trypomastigotes and revealed that they have synergistic effects, showing a promising profile for drug combination. Finally, in mice acutely-infected with T cruzi, 14 treatment significanty reduced the blood parasitaemia and had a protective effect on mortality. In conclusion, we report the identification of compounds (7), (12), (15), (23) and (26) with similar trypanocidal activity of benznidazole; compounds (9) and (21) as trypanocidal agents equipotent with BDZ, and compound 14 with potency 28 times better than the reference drug without affecting macrophages and cardiomyoblast viability. Mechanistically, the compounds inhibit cruzain, and 14 induces T. cruzi cell death by an apoptotic process, being considered a good starting point for the development of new anti-Chagas drug candidates. (C) 2017 Elsevier Masson SAS. All rights reserved.

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Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com