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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Application In Synthesis of (R)-2-Oxothiazolidine-4-carboxylic acid, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. Application In Synthesis of (R)-2-Oxothiazolidine-4-carboxylic acid, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S. In a Patent, authors is ,once mentioned of Application In Synthesis of (R)-2-Oxothiazolidine-4-carboxylic acid

Thiazolidinone compounds and composition for angina pectoris comprising the compounds as an active ingredient

A thiazolidinone compound represented by general formula (I) or a pharmacoligically acceptable salt thereof, STR1 wherein W represents sulfur or oxygen and X represents –N(R1)–, or alternatively X represents sulfur or oxygen and W represents –N(R1)–, and R1 represents hydrogen, alkyl or substituted alkyl; R2 and R3 are the same or different from each other, and each represents hydrogen, alkyl, substituted alkyl, aryl, or 5- or 6-membered heteroaryl; R4 represents hydrogen, alkyl or substituted C1 -C4 alkyl; R5 represents substituted cycloalkyl which may contain nitrogen, provided the substituents include –B–ONO2 (wherein B represents a single bond or alkylene) as the indispensable member and alkyl groups as optional members; and A represents a single bond or alkylene, has an excellent anti-anginal effect and thus is useful as an angina pectoris remedy or preventive.

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Ethanol ingestion impairs alveolar epithelial barrier function in rats

Alcohol abuse increases the incidence and severity of the Acute Respiratory Distress Syndrome (ARDS) in critically ill patients. In this study we examined a potential mechanism by which ethanol ingestion predisposes to acute lung injury by measuring alveolar epithelial barrier function in vivo as well as in cultured alveolar type II cells from ethanol-fed rats. We determined that rats fed the Lieber-DeCarli diet containing ethanol (36% of total calories) for 6 wks had decreased (p<0.05) net vectorial fluid transport, and increased (p<0.05) bi-directional protein permeability, across the alveolar epithelium in vivo compared to rats pair-fed an isocaloric Lieber-DeCarli diet without ethanol. However, ethanol-fed rats increased (p<0.05) fluid transport in response to epinephrine (10-5M) stimulation, suggesting that transcellular sodium transport was intact. In parallel, type II cells isolated from ethanol-fed rats and cultured in vitro for 6 days formed a more permeable monolayer, as reflected by increased (p<0.05) leak of 14C-inulin, compared to type II cells from control-fed rats that were cultured under identical conditions. However, type II cells from ethanol-fed rats had more (p<0.05) apical cation channel activity than type II cells isolated from control-fed rats, consistent with the preserved response to epinephrine in vivo. Finally, the alveolar epithelium of ethanol-fed rats that were supplemented with L-2-oxothiaxolidine-4-carboxylate (Procysteine), a glutathione precursor, had the same (p<0.05) net vectorial fluid transport and bi-directional protein permeability in vivo, and permeability to chronic ethanol ingestion increases alveolar epithelial permeability. Although the mechanism is unknown, it appears to involve predominantly intercellular rather than transcellular barrier disruption, and is mediated at least in part by glutathione depletion. This has important implications in understanding the pathogenesis of ARDS. One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Product Details of 19771-63-2, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 19771-63-2

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Application of 19771-63-2, 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.In a article, authors is Cacciatore, Ivana, mentioned the application of Application of 19771-63-2, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S

Carvacrol codrugs: A new approach in the antimicrobial plan

Objective: The increasing prevalence of antibiotic-resistant bacterial infections led to identify alternative strategies for a novel therapeutic approach. In this study, we synthesized ten carvacrol codrugs – obtained linking the carvacrol hydroxyl group to the carboxyl moiety of sulphur-containing amino acids via an ester bond – to develop novel compounds with improved antimicrobial and antibiofilm activities and reduced toxicity respect to carvacrol alone. Method: All carvacrol codrugs were screened against a representative panel of Gram positive ( S. aureus and S. epidermidis), Gram negative (E. coli and P. aeruginosa) bacterial strains and C. albicans, using broth microdilution assays. Findings: Results showed that carvacrol codrug 4 possesses the most notable enhancement in the anti-bacterial activity displaying MIC and MBC values equal to 2.5 mg/mL for all bacterial strains, except for P. aeruginosa ATCC 9027 (MIC and MBC values equal to 5 mg/mL and 10 mg/mL, respectively). All carvacrol codrugs 1-10 revealed good antifungal activity against C. albicans ATCC 10231. The cytotoxicity assay showed that the novel carvacrol codrugs did not produce human blood hemolysis at their MIC values except for codrugs 8 and 9. In particular, deepened experiments performed on carvacrol codrug 4 showed an interesting antimicrobial effect on the mature biofilm produced by E. coli ATCC 8739, respect to the carvacrol alone. The antimicrobial effects of carvacrol codrug 4 were also analyzed by TEM evidencing morphological modifications in S. aureus, E. coli, and C. albicans. Conclusion: The current study presents an insight into the use of codrug strategy for developing carvacrol derivatives with antibacterial and antibiofilm potentials, and reduced cytotoxicity.

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Assessment of substrate-dependent ligand interactions at the organic cation transporter OCT2 using six model substrates s

Organic cation transporter (OCT) 2 mediates the entry step for organic cation secretion by renal proximal tubule cells and is a site of unwanted drug-drug interactions (DDIs). But reliance on decision tree-based predictions of DDIs at OCT2 that depend on IC50 values can be suspect because they can be influenced by choice of transported substrate; for example, IC50 values for the inhibition of metformin versus MPP transport can vary by 5- to 10-fold. However, it is not clear whether the substrate dependence of a ligand interaction is common among OCT2 substrates. To address this question, we screened the inhibitory effectiveness of 20 mM concentrations of several hundred compounds against OCT2-mediated uptake of six structurally distinct substrates: MPP, metformin, N,N,N-trimethyl-2-[methyl(7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino]ethanaminium (NBD-MTMA), TEA, cimetidine, and 4-4-dimethylaminostyryl-N-methylpyridinium (ASP). Of these, MPP transport was least sensitive to inhibition. IC50 values for 20 structurally diverse compounds confirmed this profile, with IC50 values for MPP averaging 6-fold larger than those for the other substrates. Bayesian machine-learning models of ligand-induced inhibition displayed generally good statistics after cross-validation and external testing. Applying our ASP model to a previously published large-scale screening study for inhibition of OCT2-mediated ASP transport resulted in comparable statistics, with approximately 75% of ?active? inhibitors predicted correctly. The differential sensitivity of MPP transport to inhibition suggests that multiple ligands can interact simultaneously with OCT2 and supports the recommendation that MPP not be used as a test substrate for OCT2 screening. Instead, metformin appears to be a comparatively representative OCT2 substrate for both in vitro and in vivo (clinical) use.

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Recommanded Product: (R)-2-Oxothiazolidine-4-carboxylic acid, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. Recommanded Product: (R)-2-Oxothiazolidine-4-carboxylic acid, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S. In a Article, authors is Ishihara, Sadao,once mentioned of Recommanded Product: (R)-2-Oxothiazolidine-4-carboxylic acid

Synthesis and collateral dilator activity of nitroxyalkylamides having direct or latent sulfhydryl moieties

To develop an orally active, long-acting nitrate that does not induce tolerance, nitroxyalkyl compounds were prepared and their activities evaluated by the use of carotid collaterals in anesthetized dogs. A compound having a favorable pharmacological profile, that is, long-lasting collateral vasodilatation and little hypotension, and lack of nitrate tolerance, was chosen for further evaluation.

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Electric Literature of 19771-63-2, 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, Electric Literature of 19771-63-2, name is (R)-2-Oxothiazolidine-4-carboxylic acid, introducing its new discovery.

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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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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Total Synthesis of (+)-Latrunculin A, an Ichthyotoxic Metabolite of the Sponge Latrunculia magnifica, and Its C-15 Epimer

Latrunculin A (1), an ichthyotoxic metabolite of the sponge Latrunculia magnifica with potent inhibitory action on microfilament-mediated processes involved in cell division, was synthesized via a convergent approach.Construction of a major segment of the latrunculin backbone was accomplished by means of a three-component coupling of aldehyde 24, beta-keto ester 27, and phosphonium salt 26, which established the conjugated E,Z-diene moiety of 31.The thiazolidinone subunit of 1 was elaborated in the form of 39 from L-cysteine and was linked to 35 without nitrogen protection.Final lactonization of 47 was carried out using the Mitsunobu protocol.A parallel sequence employing the epimeric seco acid 48 produced 15-epilatrunculin A.

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Conventional and nanotechnology based approaches to combat chronic obstructive pulmonary disease: Implications for chronic airway diseases

Chronic obstructive pulmonary disease (COPD) is the most prevalent obstructive lung disease worldwide characterized by decline in lung function. It is associated with airway obstruction, oxidative stress, chronic inflammation, mucus hypersecretion, and enhanced autophagy and cellular senescence. Cigarette smoke being the major risk factor, other secondary risk factors such as the exposure to air pollutants, occupational exposure to gases and fumes in developing countries, also contribute to the pathogenesis of COPD. Conventional therapeutic strategies of COPD are based on anti-oxidant and anti-inflamma-tory drugs. However, traditional anti-oxidant pharmacological therapies are commonly used to alleviate the impact of COPD as they have many associated repercussions such as low diffusion rate and inappropriate drug pharmacokinetics. Recent advances in nanotechnology and stem cell research have shed new light on the current treatment of chronic airway disease. This review is focused on some of the anti-oxidant therapies currently used in the treatment and management of COPD with more emphasis on the recent advances in nanotechnology-based therapeutics including stem cell and gene therapy approaches for the treatment of chronic airway disease such as COPD and asthma.

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Recommanded Product: (R)-2-Oxothiazolidine-4-carboxylic acid, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. Recommanded Product: (R)-2-Oxothiazolidine-4-carboxylic acid, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S. In a Article, authors is Baruchel, Sylvain,once mentioned of Recommanded Product: (R)-2-Oxothiazolidine-4-carboxylic acid

In vivo selective modulation of tissue glutathione in a rat mammary carcinoma model

Glutathione (GSH) is known to play a role in cellular sensitivity to some chemotherapeutic agents and to radiation. Depletion of cellular GSH has been demonstrated to result in enhanced toxicity of these drugs, and this approach is being explored in the clinic as a form of biochemical modulation, using the drug buthionine sulfoximine (BSO). The fact that some drug-resistant cell lines have increased glutathione levels, and that enhancing GSH concentrations in animal tissues protects against a variety of xenobiotic agents, suggest a different potential approach to improving anti-cancer therapy. We have examined the efficacy of the cysteine ‘pro-drug’ L2-oxothiazolidine-4 carboxylate (OTZ) at enhancing normal tissue versus tumor GSH. Animals were treated with OTZ or BSO, and the concentrations of GSH in normal tissues and tumor were measured. We found that the presence of the tumor itself decreased bone marrow GSH, but that OTZ significantly increased it in this setting. Interestingly, OTZ administration significantly depleted tumor GSH levels to the same level as did BSO. OTZ could offer a selective biochemical modulation of GSH.

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