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The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof 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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The use of DHEA or at least one of its biological precursors or of its metabolic derivatives in or for the manufacture of a composition for topical application to the skin, as a pigmentation regulator for the skin or its superficial growths, especially as a depigmenting and/or bleaching agent for the skin, in particular in the treatment of pigmentation marks, and as a pro-pigmenting agent for superficial body growths.

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The Best Chemistry compound: 1,1-Dioxo-isothiazolidine

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A series of novel carbazole-containing sulfonamides and sulfamides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the results of efficacy studies in diet-induced obese (DIO) mice, and the desired pharmacokinetic parameters, compound 41 was selected for further profiling.

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A new series of benzimidazole bearing pyridine derivatives were synthesized by condensation of 1,2-phenylenediamine with 2-oxo-1,2-dihydro-pyridine-3-carboxylic acid derivative 2 in phosphoric acid to give 3-(1Hbenzo[ d]imidazol-2-yl)-pyridin-2(1H)-one derivative 3. Compound 3 on further reaction with a mixture of phosphorus oxychloride and phosphorus pentachloride gave 2-(2-chloro-) pyridin-3-yl)-1H-benzo[d] imidazole derivative 4. Moreover, 4 were reacted with different amines to give 3-(1H-benzo[d]imidazol-2-yl)-N-(substituted) pyridin-2-amine derivatives 5a-c. Meanwhile, N-(N-(substituted) sulfamoyl) pyridin-3-yl)-1H-benzo[d]imidazole-1-carboxamide derivatives 7a,b were synthesized by reaction of 5c with chlorosulfonyl isocyanate to give 2-(pyridin-3-yl)-1H-benzo [d]imidazole-1-carbonyl) sulfamoyl chloride derivative followed by reaction of the latter with different amines. On the other hand, upon treatment compound 4 with hydrazine hydrate gave the hydrazide derivative 8. The reaction of compound 8 with different alkyl/arylisothiocyanates gave the corresponding thiosemicarbazide derivatives 9a-d, while their cyclo condensation reaction with ethyl chloro acetate gave the corresponding thiazolidin-4-one derivatives 10a-c. Moreover, condensation of 10a,c with aromatic aldehydes afforded the corresponding 5-arylidine-thiazolidin-4-one derivatives 11a,b. Cytotoxic evaluation of some of the newly synthesized compounds against human breast carcinoma cell line MCF-7 revealed that, these compounds showed promising activity compared with Doxorubicin as positive control.

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Aim: A novel series of 2-arylimino-5-arylidenethiazolidin-4-ones 12a-n were synthesized and all the target compounds were fully characterized by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analysis. Materials & methods: All the target compounds were evaluated for their COX inhibition by enzyme immunoassay kit and in vivo anti-inflammatory activity. Results: Tested compounds were found more potent inhibitors of COX-2 (IC50 = 0.54-3.14 M) than COX-1 (IC50 = 4.97-11.52 M). The ulcerogenic liability of compounds 12(d, e, f, h, k, m) was performed and showed gastric safety more than or comparable to celecoxib. Conclusion: In addition, docking study of the most potent and selective compound 12h into COX-2 active site revealed that this target compound assumed interactions and binding pattern similar to that of as a cocrystallized ligand bromocelecoxib (S-58).

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Research speed reading in 2021. Quality Control of Thiazolidin-2-one, Modeling chemical reactions helps engineers virtually understand the chemistry, optimal size and design of the system, and how it interacts with other physics that may come into play. In a document type is Article, and a compound is mentioned, 2682-49-7, Thiazolidin-2-one, introducing its new discovery.

Background: The pyrrole ring is widely spread and incorporated into the structures of many naturally occurring compounds e.g. heme, chlorophyll, vitamin B12 and the bile pigments. Pyrrolnitrin and pyoluteorin are naturally occurring pyrroles which have antibiotic activity, and the methyl ester of 4-methylpyrrole-2-carboxylic acid is an insect pheromone. Moreover, the highly successful cholesterol lowering drug Lipitor is a poly substituted pyrrole derivative. Methods: Some novel pyrrole derivatives bearing other heterocyclic rings at positions-2 and -3 were synthesized and their antimicrobial activities were studied. Results: A series of novel pyrrolinthione, thiazolidinone, thiazolone, tetrazole, sulphonamides derivatives have been synthesized through a facile strategy and screened for antimicrobial activities, some of the prepared compounds exhibited high antibacterial and antifungal activities compared with the standard drugs. Conclusion: These compounds provided the impetus for most of the early work on the synthesis and reactions of pyrroles and still a very active of research. Many such explorations are anticipated in near future.

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The reaction between polystyrene 3-formylsalicylate and 2-Aminobenzylalcohol in DMF in the presence of ethyl acetate results in the formation of polystyrene N-(2-hydroxymethylphenyl)-2′-hydroxybenzylideneimine-3′- carboxylate (I). A benzene suspension of I reacts with mercaptoacetic acid undergoes cyclization and forms polystyrene N-(2-hydroxymethylphenyl)-C-(3′-carboxy-2′-hydroxyphenyl)thiazolidine-4-one, PSCH2?LH2 (II). A DMF suspension of II reacts with Mn(II) and Cd(II) ions and forms the corresponding polystyrene-anchored coordination compounds, [PSCH2?LHMn(OAc)(DMF)3] (III) and [PSCH2?LHCd(OAc)(DMF)] (IV). The polystyrene-anchored coordination compounds have been characterized on the basis of elemental analyses, spectral (IR, reflectance) studies and magnetic susceptibility measurements. II behave as a monobasic bidentate OS donor ligand in the coordination compounds. An octahedral structure for III and tetrahedral structure for IV are suggested.

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Substituted phenylsulfonamides are selective beta 3 adrenergic receptor agonists with very little beta 1 and beta 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted alkyl epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

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Chemistry involves the study of all things, chemical manipulation – in order to better understand the way in which materials are structured, how they change and how they react in certain situations. In a patent, 19771-63-2, name is (R)-2-Oxothiazolidine-4-carboxylic acid, introducing its new discovery. HPLC of Formula: C4H5NO3S

Oxidative stress due to increased formation of reactive oxygen species (ROS) in target cells of dental resin monomers like 2-hydroxyethyl methacrylate (HEMA) is a major mechanism underlying the disturbance of vital cell functions including mineralization and differentiation, responses of the innate immune system, and the induction of cell death via apoptosis. Although a shift in the equilibrium between cell viability and apoptosis is related to the non-enzymatic antioxidant glutathione (GSH) in HEMA-exposed cells, the major mechanisms of adaptive antioxidant cell responses to maintain cellular redox homeostasis are still unknown. The present study provides insight into the induction of a communicating network of pathways under the control of the redox-sensitive transcription factor Nrf2, a major transcriptional activator of genes coding for enzymatic antioxidants. Here, oxidative stress was indicated by DCF fluorescence in cells after a short exposure (1h) to HEMA, while DHR123 fluorescence significantly increased about 1.8-fold after a long exposure period (24h) showing the formation of hydrogen peroxide (H2O2). The corresponding expression of Nrf2 was activated immediately after HEMA exposure (1h) and remained constant up to 24h. Nrf2-regulated expression of enzymes of the glutathione metabolism (glutathione peroxidase 1/2, glutathione reductase) decreased in HEMA-exposed cells as a result of GSH depletion, and superoxide dismutase expression was downregulated after H2O2 overproduction. However, the expression of Nrf2-controlled enzymatic antioxidants (catalase, peroxiredoxin, thioredoxin 1, thioredoxin reductase, heme oxygenase-1) and the NADPH-regenerating system (glucose 6-phosphate dehydrogenase, transaldolase) was increased. Phenolic tert-butylhydroquinone (tBHQ), a classic inducer of the Nrf2 pathway, reduced oxidative stress and protected cells from HEMA-induced cell death through a shift in the number of cells in necrosis to apoptosis. The expression of Nrf2 and related enzymatic antioxidants downstream was enhanced by tBHQ in parallel. In conclusion, this investigation expanded the detailed understanding of the underlying mechanisms of HEMA-induced oxidative stress, and highlighted the cross-talk and interdependence between various Nrf2-regulated antioxidant pathways as a major adaptive cell response. The current results demonstrate that modulation of the Nrf2-mediated cellular defense response is an effective means for manipulating the sensitivity of cells to dental resin monomers.

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Which scientist has never heard of glutathione (GSH)? This well-known low-molecular-weight tripeptide is perhaps the most famous natural antioxidant. However, the interest in GSH should not be restricted to its redox properties. This multidisciplinary review aims to bring out some lesser-known aspects of GSH, for example, as an emerging tool in nanotechnologies to achieve targeted drug delivery. After recalling the biochemistry of GSH, including its metabolism pathways and redox properties, its involvement in cellular redox homeostasis and signaling is described. Analytical methods for the dosage and localization of GSH or glutathiolated proteins are also covered. Finally, the various therapeutic strategies to replenish GSH stocks are discussed, in parallel with its use as an addressing molecule in drug delivery.

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