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There are disclosed compounds of the formula, STR1 where n is 0, 1 or 2; A is STR2 where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R1 and R2 are independently hydrogen, loweralkyl, STR3 or aryl except that when R1 is STR4 or aryl, R2 is hydrogen, or alternatively R1 +R2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R3 and R4 are independently hydrogen or loweralkyl, or alternatively R3 +R4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

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New Advances in Chemical Research in 2021. Reactions catalyzed within inorganic and organic materials interfaces commonly occur at high coverage, causing turnover rates to depend strongly on interfacial structure and composition, In a patent, 19771-63-2, name is (R)-2-Oxothiazolidine-4-carboxylic acid, introducing its new discovery. Related Products of 19771-63-2

The effective action of endothelium-derived nitric oxide (EDNO) is impaired in patients with atherosclerosis. This impairment has been attributed in part to increased vascular oxidative stress. EDNO action is improved by administration of ascorbic acid, a water-soluble antioxidant. Ascorbic acid is a potent free-radical scavenger in plasma, and also regulates intracellular redox state in part by sparing cellular glutathione. We specifically investigated the role of intracellular redox state in EDNO action by examining the effect of L-2-oxo-4-thiazolidine carboxylate (OTC) on EDNO-dependent, flow-mediated dilation in a randomized double-blind placebo- controlled study of patients with angiographically proven coronary artery disease. OTC augments intracellular glutathione by providing substrate cysteine for glutathione synthesis. Brachial artery flow-mediated dilation was examined with high-resolution ultrasound before and after oral administration of 4.5 g of OTC or placebo in 48 subjects with angiographically documented coronary artery disease. Placebo treatment produced no change in flow-mediated dilation (7.0 ± 3.9% vs. 7.2 ± 3.7%), whereas OTC treatment was associated with a significant improvement in flow- mediated dilation (6.6 ± 4.4% vs. 11.0 ± 6.3%; P = 0.005). OTC had no effect on arterial dilation to nitroglycerin, systemic blood pressure, heart rate, or reactive hyperemia. These data suggest that augmenting cellular glutathione levels improves EDNO action in human atherosclerosis. Cellular redox state may be an important regulator of EDNO action, and is a potential target for therapy in patients with coronary artery disease.

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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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The biggest and most multifaceted class of organic compounds includes heterocyclic compounds. Currently, several heterocyclic compounds are iden-tified, and persistently gratefulness to tremendous synthetic work and synthetic usefulness, the number is increasing exponentially. In most fields of science, including medicinal, pharmaceutical, and agro-chemistry, heterocyclic compounds have a function, and biochemistry is also another area. In this research article, the green approach is administered for achieving the nitrogen, oxygen and sulphur centered five-membered heterocyclic derivatives. By taking the whole thing in to account of hetero-chemistry, the moderately effective analog for gram-positive and gram-negative bacterial strains was shown for the five-membered heterocyclic compound series of N-substituted iminothiazodine-4-one and N-(benzylideneamino)thiazol-4(5H). Throughout the synthesized series of the compound 6c revealed very much active potent against the gram-negative Escherichia coli bacterial strain and the compound 6b point out moderately active against the gram-positive Bacillus subtilis bacteria strains in accordance with the standard drug. The 5a and 6a compounds showed very strong activity against the fungal strain of Candida albicans and 6b as well as 6c were more active and highly potent than the standard drugs against Aspergillus niger species. In the view of this research drive states that all the synthesized compounds might be used for the development for further heterocyclic entities.

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Two series of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, IIIv was found to have the best in vitro inhibition activity against PTP1B (IC50 = 0.67 ± 0.09 muM) and the best selectivity (9-fold) between PTP1B and T-cell protein tyrosine phosphatase (TCPTP). Molecular docking studies demonstrated that compounds IIIm, IIIv and IVg could occupy simultaneously at both the catalytic site and the adjacent pTyr binding site. These results provide novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.

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New heterocyclic compounds are of major importance because of growing problem of bacteria and fungi resistance and antimicrobial thiazolidinone have been gaining a lot of interest. A series of Thiazolidine-4-ones derivatives as antimicrobial agent were synthesized and screened for antibacterial activity against S. aureus, E. coli and P. vulgaris and antifungal activity against A. fumigatus, C. albicans and C. albicans ATCC. The structure of the newly synthesised compounds have been confirmed from elemental analysis, IR and 1HNMR data.

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The development of new antimalarial compounds remains a pivotal part of the strategy for malaria elimination. Recent large-scale phenotypic screens have provided a wealth of potential starting points for hit-to-lead campaigns. One such public set is explored, employing an open source research mechanism in which all data and ideas were shared in real time, anyone was able to participate, and patents were not sought. One chemical subseries was found to exhibit oral activity but contained a labile ester that could not be replaced without loss of activity, and the original hit exhibited remarkable sensitivity to minor structural change. A second subseries displayed high potency, including activity within gametocyte and liver stage assays, but at the cost of low solubility. As an open source research project, unexplored avenues are clearly identified and may be explored further by the community; new findings may be cumulatively added to the present work.

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The invention provides compositions and methods for blocking the BCL6 BTB domain with small molecule, non-peptide compounds as disclosed and claimed herein. BCL6 is a transcriptional repressor of the BTB-POZ (bric a brac, tramtrack, broad complex / pox virus zinc finger) family of proteins. It is required for normal development of germinal center (GC) B-cells and is also the most commonly involved oncogene in diffuse large B-cell lymphomas (DLBCLs), and constitutive expression of BCL6 in GC B-cells causes DLBCL in mice. DLBCLs are aggressive tumors that arise from germinal center (GC) B- cells and are the most common form of non-Hodgkin’s lymphomas. BCL6 is required for survival of DLBCL cells and can limit their ability to respond to DNA damaging agents. It is also frequently expressed in follicular lymphomas (FLs), and may be required for survival of these tumors as well. DLBCL and FL collectively constitute ?60-70% of B-cell lymphomas and the incidence of these tumors has been rising in recent decades.

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New Advances in Chemical Research, May 2021. Computed Properties of C19H11F3N2O4S, Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. In a document type is Article, and a compound is mentioned, 1055361-35-7, 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile, introducing its new discovery.

Solvent-free chlorination of heteroaromatics using the phosphonium salt, prepared by reaction of triphenylphosphine with N-chlorosuccinimide, was accomplished by microwave-irradiation or heating to give the corresponding chloroheteroaromatics. Similarly, primary amides was converted into nitriles by this method.{A figure is presented}.

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An organometallic compound represented by Formula 1, an organic light-emitting device including the organometallic compound, and a diagnostic composition including the organometallic compound. wherein, in Formula 1, R1 to R12 and R19 are the same as described in the specification.

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