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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/dtmax, 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

Simple exploration of C8H10O3

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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

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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

Interesting scientific research on C3H12N6O3

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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

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Novel 2,4-dichlorophenoxy acetic acid substituted thiazolidin-4-ones as anti-inflammatory agents: Design, synthesis and biological screening

A library of fourteen 2-imino-4-thiazolidinone derivatives (1a-1n) has been synthesized and evaluated for in vivo anti-inflammatory activity and effect on ex-vivo COX-2 and TNF-alpha expression. Compounds 1k (5-(2,4-dichloro-phenooxy)-acetic acid (3-benzyl-4-oxo-thiazolidin-2-ylidene)-hydrazide) and 1m (5-(2,4-dichloro-phenooxy)-acetic acid (3-cyclohexyl-4-oxo-thiazolidin-2-ylidene)-hydrazide) exhibited in vivo inhibition of 81.14% and 78.80% respectively after 5 h in comparison to indomethacin which showed 76.36% inhibition of inflammation without causing any damage to the stomach. Compound 1k showed a reduction of 68.32% in the level of COX-2 as compared to the indomethacin which exhibited 66.23% inhibition of COX-2. The selectivity index of compound 1k was found to be 29.00 in comparison to indomethacin showing selectivity index of 0.476. Compounds 1k and 1m were also found to significantly suppress TNF-alpha concentration to 70.10% and 68.43% in comparison to indomethacin which exhibited 66.45% suppression. (C) 2016 Published by Elsevier Ltd.

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

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Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, Product Details of 593-85-1593-85-1, Name is guanidinecarbonate, SMILES is NC(=N)N.NC(=N)N.OC(=O)O, belongs to thiazolidines compound. In a article, author is Aly, Ashraf A., introduce new discover of the category.

Functionalized 1,3-Thiazolidin-4-Ones from 2-Oxo-Acenaphthoquinylidene- and [2.2]Paracyclophanylidene-Thiosemicarbazones

The reactions of dialkyl acetylenedicarboxylates with various 2-oxo-acenaphthoquinylidene- and 4-acetyl[2.2]paracyclophanylidene-thiosemicarbazones were investigated. Using simple experimental procedures, 1,3-Thiazolidin-4-ones derived from acenaphthequinone or [2.2]paracyclophane were obtained as major products in good yields. In the case of allyl derivative of acenaphthoquinylidene-thiosemicarbazones, a complex structure of tetramethyl 5-(2-(((Z,E)-N-allyl-N’-(2-oxoacenaphthylen-1(2H)-ylidene)carbamohydrazonoyl)thio)-1,2,3-tris-(methoxycarbonyl)-cyclopropyl)-4-methoxy-7-oxabicyclo[2.2.1]hepta-2,5-diene-1,2,3,6-tetracarboxylate was formed. Single crystal X-ray analysis was used as an efficient tool to confirm the structure of the synthesized compounds as well as different spectroscopic data (H-1-NMR, C-13-NMR, 2D-NMR, mass spectrometry and elemental analysis). The mechanism of the obtained products was discussed.

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

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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. 627-93-0, Name is Dimethyl adipate, molecular formula is C8H14O4. In an article, author is Khajeh-Amiri, Alireza,once mentioned of 627-93-0, Recommanded Product: Dimethyl adipate.

Microwave Assisted Highly Efficient Synthesis of Rhodanine and -2, 4-Thiazolidinedione Derivatives Under Solvent Free Conditions

Background: In the present study, we performed according to green chemistry’s standards, an easy and very efficient one-pot synthesis of2-thioxo-1,3-thiazolidin-4-one(rhodanine) and thiazolidine-2,4-dione (TZD) derivatives yin.Knoevenagel condensation of various aldehydes with rhodanine/ thiazolidine-2,4-dione in the presence of only 15 mole% of deep eutectic solvents (DESs) -choline chloride/urea- propionate and microwave radiation under solvent-free conditions Method: Twenty compounds were synthesized under thermal and microwave conditions and the yields of synthesized compounds were 77-9007O and 81-950, respectively. The IR spectra were obtained on a PerkineElmer FT-IR spectrophotometer using K.Br disks.itt NMR. and 13C NMR. of products were registered Bruker 500 spectrometer and chemical shifts are expressed as d (ppm) with tetramethylsilane (TMS) as an internal standard in.DNISO-d, as a solvent The purity of synthesized compounds was checked by chromatography and UV light (254 ran) was used for visualization. Result: A range of rhodanine and-2, 4-thiazolidinedione derivatives were synthesized using ChCll urea catalyst under solvent-free conditions at 80 C. Then, the sample derivatives were synthesized under optimum conditions Conclusion: The mild reaction conditions, good to excellent yields, easy workup, without the involxement of any harmful solvents/chemicals and easily available substrates, they all facilitated in the preparation of all synthesized compounds.

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

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Application of 14446-47-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.14446-47-0, Name is Thiazolidine hydrochloride, molecular formula is C3H8ClNS. In a Patent£¬once mentioned of 14446-47-0

Heterocyclic compounds containing nitrogen and sulfur, processes for their preparation and pharmaceutical compositions thereof

The invention relates to nitrogen- and sulfur-?containing heterocyclic compounds of the formula (I), wherein, Ar represents an optionally mono- or polysubstituted aryl or heteroaryl group;, R? represents a carbonyl or (C2 6alkenyl)-?carbonyl group;, R? represents a hydrogen atom, or a C1 6alkyl, phenyl or phenyl(C1 4alkyl) group;, R? represents a hydrogen atom or a (C1 6 alkoxy)carbonyl group;, R4 and R5, which may be the same or different, represent a hydrogen atom or a C1 6alkyl group;, R6 represents a hydrogen atom or a C1 6alkyl group or halophenyl group;, m is 0 or 1; and, n is 1 or 2,with the proviso that R? is a hydrogen atom when m is 0, and acid addition salts of the compounds of formula (I) and pharmaceutical compositions thereof. The invention also relates to processes for the preparation of these compounds. The compounds of formula (I) show a significant cerebral antihypoxic activity.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H601N | ChemSpider

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4-Thiazolidinone coumarin derivatives as two-component NS2B/NS3 DENV flavivirus serine protease inhibitors: synthesis, molecular docking, biological evaluation and structure?activity relationship studies

A series of novel 4-thiazolidinone inhibitors SKYa?SKYg, containing coumarin as a core structure were synthesized via facile and efficient method. The structures of the synthesized compounds were established by extensive spectroscopic studies (FT IR, 1D NMR, 2D NMR, LC?MS) and elemental analysis. All the synthesized hybrids were further evaluated for their potential as anti-tubercular agents against Mycobacterium tuberculosis H37Rv ATCC 25618, and anti-bacterial agents against Escherichia coli, Enterobacter aerogenes, Salmonella typhi, Streptococcus pneumoniae and Staphylococcus aureus. Interestingly, the hybrids displayed potent bioactivity. However, compounds SKYc, SKYd, and SKYe appeared to be more effective against the tested bacterial strains, among which compound SKYb showed the highest inhibition against all the bacterial strains ranging from 41 to 165?mug/mL, as compared to the standards, streptomycin, kanamycin and vancomycin. Moreover, derivative SKYa was found to be the strongest against M. tuberculosis (83?mug/mL). Additionally, the anti-dengue potential of the coumarin hybrids as two-component NS2B/NS3 DENV flavivirus serine protease inhibitors was calculated using computational molecular docking approach, with reference to the standards 4-hydroxypanduratin, panduratin and ethyl 3-(4-(hydroxymethyl)-2-methoxy-5-nitrophenoxy)propanoate with DS of ? 3.379, ? 3.189 and ? 3.381, respectively. The docking results revealed that the synthesized hybrids exhibited potent anti-dengue activity among which compounds SKYf, SKYd, SKYc and SKYe were found to be the best ones with docking scores of ? 4.014, ? 3.964, ? 3.905 and ? 3.889. In summary, we discovered 4-thiazolidinone coumarin derivatives as a new scaffold that may eventually yield useful compounds in the treatment of bacterial and viral infections.[Figure not available: see fulltext.].

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H492N | ChemSpider

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Synthetic Route of 76186-04-4, 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, Synthetic Route of 76186-04-4, name is (S)-4-Isopropylthiazolidine-2-thione, introducing its new discovery.

A acylation of the synthesis method of sulfur on behalf of the oxazolidone (by machine translation)

The invention discloses a method for acylation of the synthesis method of sulfur on behalf of the oxazolidone. Synthesis method of the invention, comprising the following steps: in the non-protic organic solvent, the compound III and under the action of an acid, the compound I with compound II carries out amidation reaction, to obtain compound IV. The method of the invention can be conducted under mild conditions, high yield, high purity, and is suitable for industrial production requirements. (by machine translation)

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H710N | ChemSpider