Simple exploration of (R)-2-Oxothiazolidine-4-carboxylic acid

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Collateral sensitivity of multidrug-resistant cells to the orphan drug tiopronin

A major challenge in the treatment of cancer is multidrug resistance (MDR) that develops during chemotherapy. Here we demonstrate that tiopronin (1), a thiol-substituted N-propanoylglycine derivative, was selectively toxic to a series of cell lines expressing the drug efflux pump P-glycoprotein (P-gp, ABCB1) and MRP1 (ABCC1). Treatment of MDR cells with 1 led to instability of the ABCB1 mRNA and consequently a reduction in P-gp protein, despite functional assays demonstrating that tiopronin does not interact with P-gp. Long-term exposure of P-gp-expressing cells to 1 sensitized them to doxorubicin and paclitaxel, both P-gp substrates. Treatment of MRP1-overexpressing cells with tiopronin led to a significant reduction in MRP1 protein. Synthesis and screening of analogues of tiopronin demonstrated that the thiol functional group was essential for collateral sensitivity while substitution of the amino acid backbone altered but did not destroy specificity, pointing to future development of targeted analogues. This article not subject to U.S. Copyright. Published 2011 by the American Chemical Society.

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Synthesis and antibacterial activity of novel 2-(arylimino)thiazolidin-4-one and 2-(benzylidenehydrazono)-3-arylthiazolidin-4-one derivatives

The ongoing spread of multidrug-resistant bacteria demands an intensive search for new antibacterial agents. In the present study, a series of new 1,3-thiazolidin-4-ones has been synthesized and investigated for its in vitro antibacterial activity. The most potent antibacterial compound 4c was found to be active, at low micromolar range, against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and the pneumonic plague causative agent Yersinia pestis with minimum inhibitory concentrations of 5 muM, 2.5 muM, 2.5 muM and 5 muM, respectively. Compound 4c showed the ability to kill E. faecalis JH212 strain with a minimum bactericidal concentration of 5 muM. Furthermore, compounds 9b and 10a inhibited the biofilm formation in S. epidermidis, where they showed 70% to 80% inhibition at a concentration of 40 muM.

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The Absolute Best Science Experiment for 19771-63-2

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METHODS AND COMPOSITIONS FOR TREATING PSYCHOTIC DISORDERS

Disclosed herein are novel drug combinations comprising a glutathione peroxidase (GPx) mimic compound and an antipsychotic agent, pharmaceutical compositions comprising one or more of such combinations, methods of preparing pharmaceutical compositions comprising one or more such combinations, and methods of treatment, prevention, inhibition or amelioration of one or more diseases associated with GPx mediated disorders, psychotic disorders or complications from administering an antipsychotic agent at high dose or long term using such combination or pharmaceutical compositions. Furthermore, a method is disclosed for reducing the antipsychotic agent’s dosages that comprises co-administering a therapeutically effective amount of a glutathione peroxidase mimic compound.

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Brief introduction of 1,1-Dioxo-isothiazolidine

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COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT

Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections

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More research is needed about Thiazolidin-2-one

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Design, synthesis and in-silico study of novel series of 2-phenyl- 3-(5-sulfanyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one derivatives with potential anti-tubercular activity

In an attempt to identify potential new agents active against tuberculosis with Shikimate kinase as the target, a novel series of 2-phenyl- 3-(5-sulfanyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one derivatives were synthesized by convenient one-pot three-component reaction of amine, aldehyde and mercaptoacetic acid on montmorillonite KSF clay as a solid acidic catalyst in good yields. The structures of the newly synthesized compounds were confirmed by IR, 1H-NMR and elemental analysis and were subjected for anti-tubercular activity by Microplate Alamar Blue Assay (MABA) against Mycobacterium tuberculosis H37Rv. Docking and ADMET studies were used to better describe the titled compounds as potential anti-tubercular agents. The compound, 2-(3,4-dimethoxyphenyl)-3-(5-sulfanyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one(4j), was found to be the most active against Mycobacterium tuberculosis H37Rv with MIC of 1.6 mug/ml and good drug likeness and dock scores. Molecular docking study revealed that the molecules fit well into the cavity of Shikimate kinase. Also, the molecular properties and bioactivity scores for the synthesized compounds obtained by in-silico studies were found to be within the acceptable range defined for human use revealing their potential as possible drug-like compounds. The anti-tubercular activity of the titled compounds was comparable to that of the standard drug Isoniazid and Ciprofloxacin. The results indicate that the synthesized thiadiazolyl-thiazolidinone derivatives may have an affinity towards Shikimate kinase active site which can be further explored for selective target based studies. Thus these compounds could act as a potential lead for further anti-tubercular studies.

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New explortion of 2682-49-7

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From fighting depression to conquering tumors: A novel tricyclic thiazepine compound as a tubulin polymerization inhibitor

A novel tricyclic thiazepine derivative, 6-(p-tolyl)benzo[f] pyrido[2,3-b][1,4] thiazepine 11,11-dioxide (TBPT), exhibits potent inhibitory effects in two non-small-cell lung cancer cell lines, H460 and its drug-resistant variant, H460TaxR, while exhibiting much less toxic effects on normal human fibroblasts. After five injections of TBPT at a dose of 60 mg/kg, it inhibits H460TaxR tumor growth in xenografted mouse models by 66.7% without causing observable toxicity to normal tissues. Based on gene perturbation data and a series of investigations, we reveal that TBPT is not a P-glycoprotein substrate and it inhibits microtubule formation by targeting tubulin, thereby causing cell cycle arrest at the G2/M stage and eventually inducing apoptosis. This redeployment of antidepressant compound scaffold for anticancer applications provides a promising future for conquering drug-resistant tumors with fewer side effects.

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Properties and Exciting Facts About 19771-63-2

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Method for 2-oxothiazolidine-4-carboxylic acid for cellular glutathione

Provided herein is a composition, method of manufacture, and method for treating a disease condition and/or raising cellular levels of glutathione, the composition comprising L-2-oxothiazolidine-4-carboxylate, (procysteine) having a purity of at least 99 to 99.5 percent.

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A new application about Thiazolidin-2-one

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Reactions of 2(3H)-furanones

This review article presents a systematic overview of approaches and reactivity data for 2(3H)-furanones, published from 1999 until 2018.

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Some scientific research about 5908-62-3

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BROMODOMAIN INHIBITORS

The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I)

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Discovery of Thiazolidin-2-one

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Targets and patented drugs for chemotherapy of chagas disease in the last 15 years-period

Background: The American trypanosomiasis, Chagas disease, is a parasitic infection typically spread by triatomine vectors affecting millions of people all over Latin America. Existing chemotherapy is centered on the nitroaromatic compounds benznidazole and nifurtimox that provide unsatisfactory results and substantial side effects. So, the finding and exploration of novel ways to challenge this neglected disease is a main priority. Methods: The biologic and biochemical progress in the scientific knowledge of Trypanosoma cruzi in the period comprising last 15-years has increased the identification of multiple targets for Chagas? disease chemotherapy. In the middle of the best encouraging targets for trypanocidal drugs, ergosterol biosynthesis pathway and cruzipain, a key cysteine protease (CP) of T. cruzi, have been pointed out. Unfortunately, recent clinical trials investigating the administration of pozoconazole and ravuconazole to chronic indeterminate Chagas disease patients revealed their inferiority compared to the standard drug Benznidazole. Results: In view of the information gained in the preceding years, a reasonable approach for the fast development of novel anti-T. cruzi chemotherapy would be focused on K777, the cysteine proteinase inhibitor (CPI) near to enter to clinical trials, and founded on the clinical evaluation of combination of known drugs with existing trypanocidal agents to obtain more efficiency and less secondary effects. Top series of xanthine have been recently identified as clinical candidate for Chagas disease. In addition, trypanothione biosynthesis, thiol-dependant redox and polyamine metabolism, the glycolytic, glyconeogenic, pentose phosphate, lipidic and polyisoprenoid biosynthetic pathways, and the enzymes from biosynthetic glycoconjugates pathways have been studied. Several specific enzymes from these particular biosynthetic pathways such as hypoxanthine-guaninephosphoribosyl-transferase and farnesyl-pyrophosphate synthase, among others, have also been broadly studied in T. cruzi. Novel synthesized anti-T. cruzi compounds with or without specific single or multi-target assigned are also described in detail. Conclusion: In summary, loans on anti-Chagas disease agents focused to specific parasite targets as their metabolic pathways or specific enzymes will be summarized. Targets will also be specifically discussed. Patent literature collected and published from 2000 to 2015, alleging inhibitors for specific T. cruzi targets or trypanocidal activity was achieved over the search database from Delphion Research intellectual property network including international patents and the European patent office, Espacenet.

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